Synthesis Of The Fentanyl Analog Beta Hydroxy Alpha Methylfentanyl First A Quick Summary:

------------------------------------------------------------------------------Synthesis of the Fentanyl analog beta-hydroxy-alpha-methylfentanyl ------------------------------------------------------------------------------First a quick summary: ---------------------Rev drone: Alright, I'm only gonna say this once... N-methyl-4-piperidone + methyl iodide ===> N,N-dimethyl-4-piperidone iodide + phenylpropanolamine, base ===> beta-hydroxy-alpha-methyl-phenylethyl-4-piperidone + aniline, NaBH4 ===> 4-anilo-1-(beta-hydroxy-alpha-methyl-phenethyl)-piperidone + (CH3CH2CO)2O ===> beta-hydroxy-alpha-methylfentanyl Next, you'll want ref's, I bet. Ho-hum. Invariably, Step 2 (the replacement of the quaternary amine with phenylpropanolamine) is the one you're wondering about, isn't it? I thought so. Chem.Heterocycl.Compd.; 21; 12; 1985; 1355-1362; You probobly want to know a little about reductive amination of aniline with your piperidone, too. Chem.Pharm.Bull.; 33; 5; 1985; 1826-1835; Just to be thorough, here's the addition of the propionyl group: J.Heterocycl.Chem.; 26; 1989; 677-686; The reasons for doing this are numerous. N-methyl piperidone is unwatched, available in big quantities, and very cheap. ------------------------------------------------------------------------------The Hive BB - Chemistry Discourse Topic: a gift from drone to the DEA -- a little china white Drone 342: Get ready for some gut-pumpin' chemical fun! As a gift from my workin' class worker bee subconscious to you, the larger community, here's a little genie that I've been struggling to keep in the bottle now for a year. "Pop", goes the cork, and like a little butterfly, this chemical nugget spreads its wings for the rest of the word. Drone's home-made fentanyl analog! Yep, drone has doen what was thought impossible, and will now divulge what is thought unmentionable, because DRONE #342 is DRONE #342, and can do that! Folks, have you ever had a hankering for a big, juicy ounce or two of synthetic heroin, but just thought it

impossible to allocate the necessary chemicals? Well, your friend drone has taken out the guesswork and managed to develope a synthetic route to a chemical 1000 or so stronger than conventional smack. Impossible, you say? NAY, my dear worker bees. Here's the general overview of fentanyl synthesis. 4-piperidone is reacted with a trimethyliodo (quaternary) salt of a phenethylamine (or any number of aromatic ethylamines), to produce an N-arylethylpiperidone (you can use the quaternary salt of the piperidone with the primary substituted arylethytlamine, if you like, too.) Anyways, this is reacted with aniline, and reduced with NaBH4, and then reacted with propionic anhydride to produce the fentanyl freebase. It turns out: *adding an ethyl carbon bridge to the piperidine ring will not reduce potency. *adding an extra methyl to the phenethyl substituent to make a phenylisopropyl makes for a strong, long-lasting compound. *adding a hydroxy to the alpha-carbon of the pehethyl side chain -- as seen in ephedrine -- will also increase potency. *as I said in a previous post, propionic anhydride can be made at home (this is the most closely watched chemical on the DEA's list, but this watching was rendered obsolete by YoursTruly not too long ago.) The Fentanyl Suite, in d(l)-major; Movement 1 (the curtain rises, our anti-hero is found quietly sauntering through the woods, foraging for precursors.) Taking this into account, Atropine is extracted from nightshade. It is hydrolyzed to form tropine. Tropine is oxidized to form tropinone. Tropinone is then exhaustively methylated with iodomethane. Second Movement Dexatrim is bought in a fiendish quantity. The PPA is extracted and isolated as its free base. This is combined with tropinone, to form N-(1-hydroxy-1-phenyl)isopropyl tropinone. (intermezzeo) Third Movement Aniline is combined with the aforementioned

freshly-made tropinone, and reduced with NaBH4. Fourth Movement (Allegro) Propionic anhydride is made from a propionate salt like calcium propionate by adding bromine or even chlorine. Alternatively, propionate esters are hydrolyzed, the acid component isolated, and combined with acetic anhydride and allowed to reflux, with the product being fractionally distilled. (crescendo) The propionic anhydride is added to our soon-to-be fentanyl analog compound, and allowed to react (I think around 50 C). The product is flash chromatographed, combined with citric acid (or any acid of your choice), and allowed to dry. The material is cut with hundreds of times its mass of mannitol. Viola! China white has just been made out of Nightshade, diet tablets, aniline, and food preservatives. It's all there in the literature. Ref's available upon request. Are we having fun yet? -drone #342 ------------------------------------------------------------------------------Rhodium (Administrator) Could we have a little more pharmacological data on this compound? I'd like to have the ref on reacting a quat with 4-piperidone, to give the tertiary amine. If you have any refs on making 4-piperidone, that would be nice too. Tropinone is easily made from citric acid, methylamine and succinic dialdehyde (made from pyrrole). You can also make cocaine from it :) ------------------------------------------------------------------------------drone 3422 - posted 05-19-98 08:50 PM ------------------------------------------------------The Robinson tropine synthesis isn't all its cracked up to be -- the main detraction is that succinaldehyde. Have you ever looked at its synthesis? At least the means that I found didn't look too appetizing; I'd extract tropines and hydrolyze and oxidize them over that any day of the week. I'll get you the ref's on this tommorow. -------------------------------------------------------------------------------

Rhodium Yes, I've looked into the synthesis. Even going the whole way to cocaine isn't that hard in my opinion. But back to tropinone. I'd very much rather make it myself, than poison myself with atropine alkaloids. Succindialdehyde is made from pyrrole by refluxing with hydroxylamine and KOH. Solomon Hey drone, thanks alot for this great stuff. Have you ever heard of PePAP (The meperidine

anolog)? acetyloxpiperidine) I think.

It's (1-(2-Phenylethyl)-4Sounds kind of interesting to me.

drone 342 Member 342] -----------

[Image] posted 05-20-98 09:43 AM [Click Here to See the Profile for drone -------------------------------------------Here's a ref or two. For the addition elimination with the quat amine, check out: Chem. Het. Comp. 21:2, (1985) 1355-1362 There's another one somewhere around in my piles of shit, butI can't find it. This one is good though, and should help you out quiite nicely. For piperidone synths: JACS 53 1931 2693, 2696 Helv. Chim. Acta 3, 1920, 815 JOC 37 1972 1042-1045 JCS 1952, 1164, 1167 Yakugaku Zasshi 71 1951 1053, 1056 JOC 10, 1945, 277, 279 JCS 1949, 708, 711 JACS 70, 1948 1820,1822 for tropinone-based fentanyls' chemistry and/or pharmacology: JMC 22, 1167 (1979) J. Het. Chem. 14, 599 (1977) Org. Magn. Reson. 6, 441 (1974) For carfentanyl: DE PAT 2610228, 1976 US PAT 4179569, 1979 Arzneim Forsch 26, 1976 1521, 1523, 1528 There, that ought keep ya busy!

-drone #342 drone 342 Member

[Image] posted 05-20-98 06:19 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Rhodium, Tropninonecan be hydrolyzed from atropine in nightshade quite easily. A little acid-base extraction, followed by vacuum distillation, will give you an excellent product for xoidizing into tropinone. Its cheap and plentiful. On top of that, its uncontrollable and essentially unlimited. However, if you do come across some really facile way of making that succinaldehyde and feel like posting it, I have some excellent ref's for some wacky benztropine analogs that put coke itself to shame (judging by the pharmacology reports and biological assays, these little goodies will pump-n-suck your dopamine receptors like you know how you want them to.) -drone #342

drone 342 Member

[Image] posted 05-20-98 08:12 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Here's some stuff from Beilstein on thebaine isolation. I actually have more at home than this, but I just couldn't get it all together this morning. Anyways, here you go: Isolation From Natural Product Isolierung aus Opium Ref. 1 761186; Patent; Knoll A.G.; US 2712018; 1951; Ref. 2 761187; Journal; Heumann; BNUNA5; Bull.Narc.; 9; 2; 1957; 34; ------------------------Isolation From Natural Product 2 of 13 Isolation From Natural Product Bldg. in Samen u. Keimlingen von Papaver bracteatum Ref. 1 3022808; Journal; Sarkany et al.; PLMEAA; Planta Med.; 36; 1979; 289; ------------------------Isolation From Natural Product 3 of 13 Isolation From Natural Product Papaver albiflorum PACZ. subsp. albiflorum Ref. 1 5559025; Journal; Slavik, Jiri; Slavikova, Leonora; Dolejs, Ladislav; CCCCAK; Collect.Czech.Chem.Commun.; EN; 46; 10; 1981; 2587-2593; ------------------------Isolation From Natural Product 4 of 13

Isolation From Natural Product Papaver bracteatum Ref. 1 3022810; Journal; Levy et al.; PLMEAA; Planta Med.; 36; 1979; 362,364; ------------------------Isolation From Natural Product 5 of 13 Isolation From Natural Product Papaver bracteatum LINDL. Ref. 1 5557634; Journal; Slavik, Jiri; Slavikova, Leonora; CCCCAK; Collect.Czech.Chem.Commun.; EN; 50; 5; 1985; 1216-1226; ------------------------Isolation From Natural Product 6 of 13 Isolation From Natural Product Papaver bracteatum Arya II Ref. 1 5910497; Journal; Meshulam, Haim; Lavie, David; PYTCAS; Phytochemistry; EN; 19; 1980; 2633-2636; ------------------------Isolation From Natural Product 7 of 13 Isolation From Natural Product Papaver fugax Ref. 1 3017192; Journal; Sariyar et al.; PYTCAS; Phytochemistry; 12; 1973; 2431,2433; ------------------------Isolation From Natural Product 8 of 13 Isolation From Natural Product Papaver oreophilum Ref. 1 3022809; Journal; Maturova et al.; PLMEAA; Planta Med.; 14; 1966; 22,38; ------------------------Isolation From Natural Product 9 of 13 Isolation From Natural Product Papaver setigerum DC. Ref. 1 6038149; Journal; Slavik, Jiri; Slavikova, Leonora; CCCCAK; Collect.Czech.Chem.Commun.; EN; 61; 7; 1996; 1047-1052; ------------------------Isolation From Natural Product 10 of 13 Isolation From Natural Product Papaver somniferum Ref. 1 64358; Journal; Parker,H.I. et al.; JACSAT; J.Amer.Chem.Soc.; EN; 94; 1972; 1276-1282; ------------------------Isolation From Natural Product 11 of 13 Isolation From Natural Product Papaver somniferum Ref. 1 163865; Journal; Barton,D.H.R. et al.; JCSOA9; J.Chem.Soc.; EN; 1965; 2423-2438; ------------------------Isolation From Natural Product 12 of 13 Isolation From Natural Product Papaver somniferum Ref. 1 5829983; Journal; Waddell, Thomas G.; Rapoport, Henry; PYTCAS; Phytochemistry; EN; 24; 3; 1985; 469-472; -------------------------

Isolation From Natural Product 13 of 13 Isolation From Natural Product Papaver somniferum after extraction with aqueous sodium bisulphite, removing morphine and codeine and extraction with acetic acid Ref. 1 5856249; Journal; Repasi, Janos; Hosztafi, Sandor; Szabo, Zoltan; PLMEAA; Planta Med.; EN; 59; 5; 1993; 477-478; drone 342 Member

[Image] posted 05-20-98 08:33 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Sorry about that; this last message belongs in the current opium thread in the novel discussion area. imagine my chagrin, -drone #342

Rhodium Administrator

[Image] posted 05-24-98 08:19 PM [Click Here to See the Profile for Rhodium] ------------------------------------------------------Succinaldehyde [JACS 68, 1608-1610 (1946)] Various procedures, usually applicable for the preparation of aldehydes from appropriate intermediates, were tried unsuccessfully: e. g., the distillation of mixed calcium succinate and calcium formates, a Rosenmund type of reduction of succinyl chloride, the partial hydrogenation of succinonitrile, either catalytically or by Stephen's methods with stannous chloride, to the diimine; all gave no trace of the desired aldehyde. Bromo- and chloroacetal do not undergo the Fittig condensation, but instead yield ethyl vinyl ether. The Grignard condensation of beta-halogenopropionaldehyde acetal with ethyl orthoformate, expected to yield the tetraethyl acetal of succinaldehyde, was not tried since neither beta-chloro- nor beta-bromopropionaldehyde acetal would react with magnesium. Hence, resort was made to the synthesis of succinaldehyde from pyrrole, via the dioxime, and a procedure was employed which does not require the isolation of the dialdehyde. Succinaldoxime In a 2-liter, 3-necked flask, equipped with mechanical stirrer and reflux condenser, were placed 1 liter of ethanol, 67 g freshly distilled pyrrole, and 141g hydroxylamine hydrochloride. The mixture was stirred and heated to refluxing, as soon as solution was complete 106g anhydrous sodium carbonate was added, in small portions, as rapidly as possible; and the solution was then refluxed for-twenty-four hours. The hot alcoholic mixture was then filtered to remove sodium chloride, and the filtrate was evaporated to

dryness under reduced pressure. The residue was taken up in the minimum of boiling water, the solution heated with decolorizing charcoal, filtered and the product allowed to crystallize in the refrigerator. Additional product could be obtained by concentrating the mother liquors. The yield of dioxime varied from 40 to 44g, 35 to 38%, and the product melted at 171-172�C. Succinaldehyde A twentieth mole, 5.8g, of succinaldoxime was placed in a beaker of 250 ml. capacity and 54 ml. of 10% sulfuric acid was added. The mixture was cooled to 0�C and to it was added, in small portions, 7.0g of sodium nitrite, keeping the temperature at 0�C. Evolution of nitrogen dioxide fumes indicates too rapid addition of the nitrite. The dioxime was now completely dissolved, and the solution was allowed to warm slowly to 20�C and effervescence to go to completion. The lemon-colored solution was then neutralized to litmus by the addition of small portions of barium carbonate, and the precipitated barium sulfate was removed, leaving the free succinaldehyde in the filtrate. The solution was assayed at this point by precipitating quantitatively from an aliquot portion the bis-2,4-dinitrophenylhydrazone; the weight of crude derivative showed that consistent yields of 90% of the dialdehyde could be expected. Since this solution was found satisfactory for these studies, the aldehyde was not isolated, thus avoiding loss of product. The bis-dinitrophenylhydrazone, after recrystallization from alcohol, melted at 278-280�C. Succindialdoxime [JOC 21, 644-647 (1956)] Hydroxylamine hydrochloride (90.5 g., 1.30 moles) was pulverized and stirred 30 minutes at room temperature with alcohol (400 ml). A solution of potassium hydroxide (44.8 g, 0.8 mole) in water (50 ml.) and alcohol (50 ml) was added. To the thick mixture pyrrole (34.5 ml, 0.5 mole) was admitted and the whole was refluxed gently for 23 hours, during which period it gradually turned orange-brown and gave off ammonia. Alcohol (100 ml) was added, refluxing continued another hour, and the mixture was filtered hot with suction. The inorganic residue was washed white with hot alcohol (100 ml), and the dark filtrate and washings were concentrated under vacuum to a tan semi-solid which was collected and washed with a little alcohol: 56 g. When treated with 18 N sulfuric acid, the vacuum distillate turned bluish-green and deposited hydroxylamine hydrosulfate (1.8 g). The filtrate and washings, which had an odor reminiscent of indole, containedtarry impurities and hydroxylamine hemichloride (~8 g). The tan residue (56 g) was mixed with an equal weight of water (endothermicity!) and, after a half hour, the water-soluble impurities (ammonium chloride and

hydroxylamine hemichloride) were filtered off leaving 35.5g (61%); This product ras recrystallized by addition of six times its weight of boiling water, swirling occasionally until dissolved, adding Darco (4g), and filtering after 2 minutes through Super-Cel with suction. The yellow filtrate soon deposited crystals and, after storing 2 days at 5�C, the succindialdoxime was collected; 30.4 grams (52%) of pale yellow crystals, mp 169-170�C. Osmium Member

[Image] posted 05-26-98 04:58 AM

Piglet Member

[Image] posted 05-26-98 10:14 AM

[Click Here to See the Profile for Osmium] ------------------------------------------------------Give us your coke analogue refs, drone. Please.

[Click Here to See the Profile for Piglet] ------------------------------------------------------While we are on the subject of potent analogues, can anyone comment on the cocaine analogue with a P-Fluoro group on the benzoic acid ? the Future Synthetic Drugs of Abuse says that it is 60 times stronger than the parent compound. Many moons ago I suggested that this could be made by purchacing cocaine, purifying it and converting it to ecgonine using CaO and then reacting it with HCl/Methanol to get the methyl ester & then Para Fluoro Benzoic Acid. The PFBA could be made from Para Amino Benzoic Acid (health food shop!) via NaNO2 to produce the diazonium salt and then reaction with sodium fluoroborate or fluoroboric acid (careful!). Fluoroboric acid can be made from hydrofluoric acid & boric acid. You can't use glass for this bit & the fluoride WILL send you to an early grave if you make a mistake. Ammonium flouride can be purchased to clean concrete off glass & for glass etching. drone 342 Member

[Image] posted 05-26-98 10:49 AM [Click Here to See the Profile for drone 342] ------------------------------------------------------for benztropine analogs that are fun: US Pat 2799680 (1954) US Pat 2706198 (1952) JMC 37, 15, (1994 2258-2261 JMC 38, 20, (1995)3933-3940 for JMC JMC JMC JMC JMC JMC

CIT 34, 34, 35, 35, 36, 36,

and other coke-esque analogs: 10, (1991) 2719-2725 10, (1991) 3144-3146 13, (1992) 2497-2500 25, (1992) 4764-4766 7, (1993) 855- 862 20, (1993) 2886-2890

JMC JMC JMC JMC JMC JMC

37, 37, 37, 37, 38, 38,

8, (1994) 1220-1223 10, (1994) 1535-1542 11, (1994) 1558-1561 18, (1994) 2865-2873 2, (1995) 379- 388 16, (1995) 3086-3093

This is an incomplete list; I have a stack of xeroxes of articles realted to these chemicals that's about 3 inches thick. Turns out, if you wire the phenyl group directyly to the tropane ring (no oxygens or carbonyls, or whatever), potency increases. In addition, it apprears the general rule is that substituents on the 4-position of the phenyl generally increase potency. As for benztropine, it turns out that if you add halides on its phenyl groups at the 4-position, you get something much more selective for dopamine, and much less of an anticholinergic, which translates to a better (higher) ratio of tweak:wierdness than coke. This is one of my last posts for a long time, so I hope this helps out. Keep up the good fight. -drone #342 336669 Member

[Image] posted 07-20-98 05:09 PM

drone 342 Member

[Image] posted 07-21-98 11:03 AM

[Click Here to See the Profile for 336669] ------------------------------------------------------wow! you guys really know your stuff, huh? I'm impressed!

[Click Here to See the Profile for drone 342] ------------------------------------------------------Piglet, here are actually analogs of that cocain derivative that are even STRONGER. I'm awat from my ref's, but if you look up that fluorophenylecgognine analog using Beilstein, it'll list many more articles covering them. -drone #342 drone 342 Member

[Image] posted 07-21-98 11:06 AM [Click Here to See the Profile for drone 342] ------------------------------------------------------336669, thanks. I'm glad our work is appreciated. I've always felt that fentanyls could act as sort of the heavy artillary of the WOD's. Considering thier dosage size, and the materials they can be made out of they're unstoppable (look what a problem speed is, now imagine a drug with a dosage *SEVERAL ORDERS OF MAGNITUDE SMALLER*!)

BOZAKIUM

[Image] posted 07-21-98 04:27 PM

[Click Here to See the Profile for BOZAKIUM] ------------------------------------------------------shit! this thread made me bust a nut in my pants!!! I have always wanted a good lead on the fentanyls, and y'all bees have opened the door for me. Thanx. For the money people out there, a pound of methyl fentanyl is worth over a bilion dollars. It would be great for someone to do a PIHKAL-type project on all the fentanyls AND coke analogues.mmm-mmm. The Alchemist Member

[Image] posted 07-22-98 08:25 PM [Click Here to See the Profile for The Alchemist] ------------------------------------------------------I would love to dream up some methyl-fetanyl but there's always that old story of the MPTP byproduct. Under what conditions is this byproduct made and what's the best way to keep it out? Clueless on the fentanyl scene but mmmmmmm... does it sound yummy. -the alchemist

drone 342 Member

[Image] posted 07-24-98 09:37 AM [Click Here to See the Profile for drone 342] ------------------------------------------------------Boz, A HardDrug-iHKAL-thingy is already in the works! MTPT is not a byproduct from fentanyls, but rather from some extremely potent pethidine analogs. Both opioid agonists, but I never understood why one would rather make pethidine over fentanyl. It was the result of high temps and/or low pH's at a particular step, but don't quote me on that. The most important thing here hygene. This stuff is extremely potent, and the last thing you want to do is accidentally breath in a milligram while working with it. -drone #342

Osiris Junior Member

[Image] posted 07-25-98 04:13 PM [Click Here to See the Profile for Osiris] ------------------------------------------------------Drone, these fentanyls sound very interesting. Unfortunately, I do not see them taking over the world, due to the fact that they are so powerful. In the LSD world, the chemist can produce liquid and just pass it down to the people farther down the chain for them to cut and/or soak into blotter paper. I am assuming that the entanyls would be primarily distributed via blotter also. If one of the

distributors fucks up and accidentally makes blotter without cutting and each blotter has 1 mg LSD, the unwitting ingestors will trip very hard but since it is impossible to OD on LSD with anything anywhere close to a normal dose, they will still be physically safe. Make a similar mistake with fentanyls, though, and people will be dropping like flies, right? That sort of thing tends to put people off your product. To avoid this possibility, the chemist will have to make up the blotters himself. If the chemist makes up ten million doses of his fentanyl, that means that he has to dip one hundred thousand blotter cards himself. Even if our chemist can come up with a way to do this more quickly and easily, he still has to figure out a way to purchase 100,000 blotter cards without drawing a lot of heat. And then he has to figure out how to MOVE all of that bulky paper. I have never been involved with anything of this nature, so this is all speculation and I might be wrong. If so, please correct me. It would be cool if massive fentanyl manufacturing, packaging and distribution could be made to work well - if nothing else, it would keep a lot of addicts from having to stick needles in themselves many times a day to get their fix, which would be a huge boon to overall public health. bootie rocket

[Image] posted 07-25-98 05:54 PM [Click Here to See the Profile for bootie rocket] ------------------------------------------------------Perhaps it could be dissolved in a solvent and sprayed on an inactive powder and snorted. I'm not into H or it's derivitives but I can think of the way most H masters I've seen prefer to do it, and it aint snorting;) You sick little monkeys, I love ya! -BR

ICEKAT Member

[Image] posted 07-26-98 05:00 PM [Click Here to See the Profile for ICEKAT] ------------------------------------------------------Hello ALL, I participated in a study at the univestity s departmant of anesthesiology with fentanyl and let me tell you it is a potentially very very dangerous drug. I say that because I know first hand. It has some some terrible side affects like at high doses riggitity and contraction of muscles, plus a not to unpleasant itchie eyes, nose, and back. You feel great at first but I at a very high dose decided I didn't need to breath. I was so out of it the staff had to shake me and tell me to remember to breath. I would then remember and breath but soon forget again until I became completly unresponsive and had to be resperated

and brought down. I did this two times. And was artificialy resperated both times. The nausia is terrible, and Dry heaved twice even though I had fasted and no liquids and I felt terrilble. This drug is for only the most responcible of types because dosage is very very very very very critical. I was lucky enough to get the experience in a very controled stetting with a group of trained profesionals working to make sure everything would be ok. A little oops and say goodbye cause your going to forget to breath. I would suggest selling Naloxone (SP?) with any and all that gets on the streat because that is one of the only drugs to bring you down in case of overdose. Or a automatic resperator would work well to. BECAREFUl!!!!!!!!!!!!!!!!!!!! ICEKAT drone 342 Member

[Image] posted 07-26-98 06:19 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Osiris, I see what you mean, but this is not the case. Fentanyl would obviously be mixed with something like mannitol to dlute it to a more manageable size. Why would anybody want to do blotter smack? In any case, you're worried about some dealer fucking up with measurements -- which is a reasonable concern. However, with fentanyls, its actaully SAFER than other comparable drugs. The therapeutic index for fentanyls is much higher than for heroin, so that you actually have a safer product. There's a wider safety margin with fentanyls than with opiates or any other opioids -- making this more ideal than other products. Moreover, the general trend with them is that as the potency increases, so does the ratio between getting fucked up and ODing. In a certain sense, by providing this product, a dealer would be offering a safer, cleaner, healthier alternative to the shit on the street -- you just might be *saving* lives! ;) In any case, the amount of impurities would be greatly diminished (let's not get nuts here; nobody'll get any humanitarian awards for distributing synthetic smack, even if it meant less overdoses, which is certainly debatable!) BootieRocket has the right idea here of what could be done. This idea also came to me. Yes, Bootie, we are sick. Sick, sick, sick. I have to say that what Icekat is saying is true -what he described is a textbook example of an opiate overdose. However, I'd also add that it's no more

dangerous when it comes to dose-sizing than heroin -in fact its somewhat safer. A massive dose of just about any opioid agonist will give the effects that Icekat described. Naloxone is not something you want to give to heroin addicts. Wanna see a pretty freaky death? Watch what happens when you give 'em an opioid antagonist -"landflounder" is the name that comes to mind immediately. Anyways, this would be a great way of putting certain countries out of business (or at least give them a run for their money)-- Burma, Nigeria, Laos, Afghanistan etc. Imagine the regional chaos when the one commodity that bolsters the economies and dictatorships of so many parts of the world becomes far cheaper and easier to make "at home" than they possibly could afford to do the conventional way. -drone #342 drone 342 Member

[Image] posted 07-26-98 06:21 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Also, before I forget. Sasha IS NOT putting together a book on this stuff -- a little German elf friend of mine is. I realized that my comments might look a little confusing. -drone #342

Osiris Junior Member

[Image] posted 07-27-98 01:30 AM [Click Here to See the Profile for Osiris] ------------------------------------------------------Drone, people would want to do blotter smack for the same reasons that people want to do blotter LSD: you can be sure it isn't cut with something dangerous, you don't have to stick needles in your flesh or snort/eat bad-tasting powder, you can be reasonably sure that the dosages are roughly the same per batch, and the look of the blotter paper provides an excellent way to easily determine the potency/quality of the drug and which batch it came from. You just suck on a tiny piece of tasteless blotter paper for half an hour and then spit it out. Suppose you mixed your fentanyl with mannitol, like you said. Can you be sure that there aren't any isolated bits of pure fentanyl that didn't get adequately mixed? Everyone, no matter how competent, makes a mistake every now and then. Can you vouch for the cutters farther down the line as well? Or suppose I don't like to snort or slam mannitol or other filler substances and I am used to purifying my street shit before I use it. I can't do that with fentanyl because

I'll be lucky if I can *see* the pure drug when all the cut is gone! Although I am not into opiates, I would probably try fentanyl on blotter (once) if it was offerent to me. There is NO FUCKING WAY IN HELL I would ingest fentanyl in powder form. Too risky, especially considering that it looks much easier to make fentanyl than LSD and therefore the competence of the cooker could easily be much lower. If you were the chemist I'd probably trust you to have done things correctly, but out on the street you don't usually know these things and the risks are simply too great. As far as the ED/LD ratio, is it high enough that if someone slams a couple mg of powder which is 90% fentanyl instead of 0.5% (or whatever) they won't die? I doubt it, although you are the expert here. This could easily happen if the chemist lets any pure product get out of his lab and it is cut improperly by some know-nothing backstreet dealer. Thus, your chemist has to cut the shit out of his stuff before he sells it, thus multiplying enormously the quantities of material he has to move and thereby negating one of the few things that work in a chemist's favor - that he can sell pure product in a less bulky form. I don't mean to rain on your parade and you are the expert on the drug itself and I know nothing about fentanyls except what you have posted on The Hive, but I honestly don't see distribution on anything but blotter as being workable. With blotter the chemist has the hassle of having to prepare all the doses himself, but at least he isn't leaving it up to people who either don't know or don't care about how to properly handle such incredibly potent drugs. You have let the cat out of the bag with your detailed new methods of fentanyl production. If your methods are as easy as you say they are, they will leave the Hive and show up on the street because the smack market is so very lucrative. I would hate to have this new market start off with hundreds of OD deaths before a safe way of ensuring dosage consistency starts being used. If the people that are undoubtedly reading this right now and are planning to set up fentanyl labs start from scratch with use of blotter paper as a dose distribution mechanism, hopefully those hundreds of ODs will never have to happen. Fentanyl chemists/dealers will certainly not win any official humanitarian awards, but if they can convince hardcore addicts to switch from AIDS-spreading needles to harmless blotter tabs, I think a great good will have been done. As well, if tens of millions of doses of fentanyl can be cooked up without LSD-level difficulty, the overall street price should come WAY down due to dealer competition and maybe more addicts

will be able to afford their fixes without having to make a living as thieves, dealers or prostitutes. I think those are quite noble goals, as is the goal of taking the production of opiates (and hopefully cocaine too, someday) away from third world countries who cannot hope for political stability as long as the incredibly lucrative drug trade poses such a pervasive corrupting influence. This thread is without a doubt the most important topic that has yet come up on the Hive. In fact, it is the most important topic I have seen come up since I started reading the original alt.drugs in 1990. These hyperpotent synthetic analogues of heroin and cocaine have the potential to change the world to such an extent that I am finding it difficult to grasp the sheer scale of it. Realignment of the foundations of the Heroin and Cocaine trade will topple governments and criminal empires. Given that what is said on The Hive almost certainly makes it way to the ears of those who control these empires, they'll certainly perceive you as a threat to their profits and try to eliminate you and anyone else you are working with before you can make any further advances or publish that book. You had better make sure that your internet anonymity is absolutely uncompromiseable. Better get a Nymserver account from the Lycaeum instead of your current hotmail account, and invest in a subscription to a TCP anonymizer while you are at it. You need to assume that these people have the resources to buy phone taps and traces, pay hackers to sniff packets everywhere looking for the string "Drone 342" and to break into any systems that they need to to acquire this information. They could bribe or threaten the managers of Wolfe.net (The Lycaeum's upstream internet service provider) to allow them to sniff every packet that enters or leaves the Lycaeum. They could do the same to Hotmail, which logs all TCP connections. These people will not be worried about their evidence being admissible in court, they will not have to operate within the law to get their information, and they have enough money to buy God. They won't want to arrest and prosecute you, they will want to kill you. And right now you are the single biggest threat to their money and power. If the speculators about the CIA's drug running are correct, this will also put a severe crimp in *their* cash flow, and if you don't want to piss of the drug cartels, you REALLY don't want to piss of the spooks. The spooks can find anyone, anytime, anywhere and take them out with surgical precision. That is their job. And they work hand-in-glove with the NSA, who analyze every single packet that flows over the internet.

Worldwide. They are almost certainly going to read this. Hi, guys! No, I am not posting this in the middle of a meth psychosis. I am completely sober. If you aren't scared yet, you are a fool. I am pretty fucking scared myself. If you continue to work on making syntheses of cocaine and heroin analogues easier, I suggest you cut all societal contacts and move to somewhere very remote to continue your work. You MIGHT be safe enough if you use the Nymserver and a TCP anonymizer, but I can't guarantee that those resources haven't been co-opted by the spooks as well. Good luck in whatever you choose to do, Drone. You'll need it. First off, thank you for the kind words. I've given this action a lot of thought, and I felt it very necessary to the right thing by letting the world know. You said: "Fentanyl chemists/dealers will certainly not win any official humanitarian awards, but if they can convince hardcore addicts to switch from AIDS-spreading needles to harmless blotter tabs, I think a great good will have been done. As well, if tens of millions of doses of fentanyl can be cooked up without LSD-level difficulty, the overall street price should come WAY down due to dealer competition and maybe more addicts will be able to afford their fixes without having to make a living as thieves, dealers or prostitutes. I think those are quite noble goals, as is the goal of taking the production of opiates (and hopefully cocaine too, someday) away from third world countries who cannot hope for political stability as long as the incredibly lucrative drug trade poses such a pervasive corrupting influence." You also said: "These hyperpotent synthetic analogues of heroin and cocaine have the potential to change the world to such an extent that I am finding it difficult to grasp the sheer scale of it. Realignment of the foundations of the Heroin and Cocaine trade will topple governments and criminal empires." ...And that is exactly why I had to let this information out. I couldn't have said it better. Yes, I am concerned a bit for my own annonymity, privacy, and freedom. However, I've ALWAYS posted from public terminals annonymously. While the Powers-That-Be could certainly find me out if they REALLY tried, I'll just take my chances. If this

spreads, it was worth it. If not, then I'm safe. Anyways, back to nuts-and-bolts. Originally, I was skeptical of the blotter packaging idea, but now I see its advantages. While I'll stand by powder for personal snortin' reasons, blotter is the way to go for "The Masses". For safety, eating the shit is best, but eating it will pretty much eliminate The Rush -the whole point to smack in the first place! It also means feeling A LOT sicker. The reason people snort and shoot smack is because the reward is immediate and overpowering. With eating, you have to wait a bit, and why wait? However, by soaking the blotter tab in 0.5 mL of H2O, you have your fentanyl in shootable form (or a sort of nasal spray.) This means that this form would be neatly dosed -- far moreso than conventional H, and guarunteed uncut. Such a form would have its own sort of mark of quality, and would ensure a greater degree of safety for the user. -drone #342 ketone Member

[Image] posted 07-30-98 10:36 PM [Click Here to See the Profile for ketone] ------------------------------------------------------Drone: the birth of a new designer drug ;-) Excellent work...thanks for sharing and I commend you for your guys and hard work! -ketone

Osiris Junior Member

[Image] posted 07-30-98 11:51 PM [Click Here to See the Profile for Osiris] ------------------------------------------------------Drone, you are a man of conviction. Such are rare in today's world, especially among drug chemists (not to suggest that you are one of those, just a random point y'know). I admire your courage. Good to see that you are taking your internet security seriously. I guess I went a little bit overboard with the paranoia in my previous post, but I thought about it a bit and came to the following conclusion: drug lords probably won't have the technical acumen to be able to track you down if you take precautions (and it sounds like you are), and if the spooks wanted you you'd already be dead. Besides, like you said, all that fentanyl stuff is already out there in the literature, right? Whacking you wouldn't solve anything. But it will be very interesting to see what the cartels will do when fentanyl starts hitting the streets. Will they cut their prices? Will they give up? Will they start producing fentanyl themselves? Interesting times a-comin.

I like your idea about treating the blotter tabs as a universal dose "package". The nasal spray idea is killer! People could "shoot up" in public and no one would know! You could maintain a habit and still have a normal life - just tell everyone that you have chronic sinus problems |->. I have heard of people doing this trick with cocaine in saline solution - one puff up each nostril and you have the equivalent buzz of a couple cups of coffee, without the jitteriness of caffeine and without a gutful of bitter liquid. Less addictive than snorting lines or smoking base, too efficient doasge titration is a major key to avoiding tolerance and addiction. Now, the blotters will need to be printed with a distinctive logo to eliminate any possibility of confusion with LSD tabs. I suggest a little needle that should get the point across |->. The logo should be sized to fit on one tab so if the tabs are broken up and somehow mixed up with LSD tabs, they can still be readily identified. That is probably pretty unlikely, but better safe than sorry. The blotter pattern could be customized on a per-batch basis by varying the color and/or color pattern of the background and/or the logo. Junkies have historically looked down on psychedelic drugs and LSD in particular. Given this, it'll be funny as hell to see fentanyl users saying things like "man, those aqua tabs were the BEST! They were soooo clean..." or calling certain batches "triple-dipped" |->. Rhodium Administrator

[Image] posted 07-31-98 08:31 AM [Click Here to See the Profile for Rhodium] ------------------------------------------------------When will we get a step-by-step "recipe" for the production of OTC fentanyl analogs here? Such a text would get a special place on my chemistry page. It is always fun to change the world as we know it ;)

Bright Star Member

[Image] posted 07-31-98 09:08 AM [Click Here to See the Profile for Bright Star] ------------------------------------------------------Thank you drone for not being scared off. Osiris put the 'willies' in me for a while... but after all, the information should be available. But then again, I'm the paranoid type. And even if these analogs become available... It definatly would be a liquid, with the fentanyl dissolved in it. A little shacking and everyone is assured of a common dosage. Bright Star

Lump

[Image] posted 07-31-98 04:38 PM [Click Here to See the Profile for Lump] ------------------------------------------------------Hope you guys make this a reality. Well do I remember the last big batch of fentanyl analogues to hit the East Coast. It was around 1992/93, and I believe the material was 3-methyl-fentanyl. It was MUCH better than plain vanilla fentanyl -- lasted every bit as long as heroin and felt identical from rush to nod to dopesickness. The stuff was all over the streets for awhile and killed a couple of friends of mine. IT CANNOT BE CUT IN THE USUAL WAYS WITH POWDER. I was very happy to see the above suggestion of blotter, as I'd been thinking of that since those noddy days. By the way, does anyone know anything about George Marquart (sp??). I know he's rotting away for producing much of the super-fent this country has seen, but never learned much about him.

Osiris Junior Member

[Image] posted 07-31-98 11:49 PM

Cyclops Member

[Image] posted 08-03-98 09:51 AM

[Click Here to See the Profile for Osiris] ------------------------------------------------------I read about Marquat in Newsweek when he was busted. They said he was supplying the entire east coast with fentanyl, was a reclusive super-genius chemist, and acted alone. Wierd guy - when the judge asked him what type of chemist he was, he said "clandestine" |->. I'm sure that didn't reduce his sentence any...

[Click Here to See the Profile for Cyclops] ------------------------------------------------------Funny you should mention Marquart. He was on an episode of "The Justice Files" just last weekend. Very unapolgetic too, he was. The producers of the show called him a mass murderer...such audacity! He was givin' the people what they wanted. Another featured on the same show was J. Dahmer, one who gave nothing to anyone, while taking all. Shameless non-sequitur. drone 342 Member

[Image] posted 08-03-98 10:27 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Rh, A fentanyl synth with all its gory details is underway. Puttin together something as involved as a fentanyl "recipe" is hard work, and takes a lot of time -- especially now that I don't have OCR capabilities anymore! Originally, this was something I was hoping to have published, and I'm still thinking about it. I've managed to compile information that has eluded

almost everyone, and it does feel a little wierd just *giving* it away. Still, my beliefs drive me to do something liek this. This whole writing process may take a while. -drone #342 Shaft Junior Member

[Image] posted 08-06-98 01:55 AM [Click Here to See the Profile for Shaft] ------------------------------------------------------Drone 342: I feel that it may not be my place to say, but giving this recipe away is a very generous act. Alot of people harbor the idea that there is a marked line between opiates and other drugs due to their strength, and possibility of withdrawls or whatever. So a bold act could be to publish this book on "hard" drugs, and distribute recipes freely on the fentanyl analogues. It's definately not my place to say, but I say go for it. I, for one, think maybe a little segment could be set aside for synthesis of these compounds; with troubleshooting tips, recipes, and further.

saint_nicholaus [Image] posted 08-10-98 11:37 AM [Click Here to See the Profile for saint_nicholaus] ------------------------------------------------------what up gang? short reply on blotter paper issue. if fentanyl is water soluble you could drop blotter in a rig and go to it i have seen it done with LSD and DH2O. onset was instintaneous or about 3 seconds, duration of peak was diminished to about 4 hours from 8, affect still hung out for about 24 hours such as dialated pupils and general tweeked pespective. chris. Kaff Member

[Image] posted 08-20-98 03:36 AM [Click Here to See the Profile for Kaff] ------------------------------------------------------I know absolutely nothing about fentanyl anoalogs in fact I never even heard of them before, but they sound really incredible. I never knew that there are synthetic drugs stronger than heroin and cocaine. Yes, definitely a great idea to get recipes for this. I think also we should work on the microwave chemistry aspect, as mentioned on Rhodium's page. Microwaves seem to have the potential to increase yields and save time. How about a bunch of chemists collaborating on a really thick book- the drug version of "The Joy of Cooking". A book the size of a big real cookbook.

drone 342

[Image] posted 08-22-98 05:28 PM

Member [Click Here to See the Profile for drone 342] ------------------------------------------------------Progress report: This synthetic description is taking way too much time. However, progress is being made, and new chemical insights are being discovered. Yes, fentanylsare pretty amazing. However, these still aren't the strongest recreational drugs of all; in my studies I've seen a few things active at the sub-nanomolar level that may or may not be worth investigating. Can't remember much about these chemicals, but I'll dig through my notes on it. -drone #342 Kaff Member

[Image] posted 08-22-98 11:04 PM

Piglet Member

[Image] posted 09-02-98 05:45 AM

[Click Here to See the Profile for Kaff] ------------------------------------------------------Imagine using genetic engineering to add the drug-components from marijuana or opium poppies to other plants like apple trees or tomatoes so we'd have fruits and vegetables containing THC and opium.

[Click Here to See the Profile for Piglet] ------------------------------------------------------D342 & Shaft: Direct yourselves to US patent 3,905,981 which describes the cleavage of tertiary amines and a route to replace the N-Methyl with other substituents at 75% yield. -OH groups need to be protected. As I see it. 1. Convert codeine to hydrocodone a la rhodium method. 2. Replace N-Methyl with N-phenyl ethyl using methyl chloroformate (DIY from ethylene glycol and phosgene (careful!!). 3. Remove methyl ester with HBr in CH3COOH. This should yield about 30%. Your product is about 100 times stronger than morphine. As strong as 3-methyl and somewhat simpler to do (I guess). Criticism please, Piglet :) Piglet Member

[Image] posted 09-02-98 08:45 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------Actually, I think that there are n-substituents that are stronger than PE. Rhodium's page has links to some of the research centers for these things.

Also, I think replacing that 6 =O group with other funky things has quite an impact on the agonist strength. =CH2 is 80 times stronger than -OH but a bitch to get in. I seem to remember than amino groups appear in some of these things. Check the RBI... Piglet :) drone 342 Member

[Image] posted 09-02-98 07:49 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------Piglet, Thanks for the tip on the tertiary amines substitution; I'll give that a thorough investigation. Right now I'm looking into just that issue, since when Tropinone does what I said it would do, there is a place in the mechanism where it does violate Brett's rule -- though there are examples of tropinone methyliodate succesfully getting away with doing such a thing. More research needs to be done here. -drone #342

Kaff Member

[Image] posted 09-03-98 04:20 PM [Click Here to See the Profile for Kaff] ------------------------------------------------------Strike says the war is over on the back cover of Total Synthesis. The war isn't ever over but it would be nice to have a book on the more advanced drugs such as China White. Just out of curiosity, what are the main precursors of this dessert? Sounds better than Russell Stover-Fanny Farmer- Whitman-Laura Secord-Tobler Swiss milk chocolate!!!

Piglet Member

[Image] posted 09-05-98 08:40 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------Could I also suggest some bits? 1. Naloxozine 'potent u1 receptor antagonist'. I won't bore you with the full name but imagine 2 Oxymorphone molecules with an N-allyl group (antagonist) on each N and the two are bonded by a hydrazide at the 6 positions. I wonder how srtong an agonist this would make? Not impossible to make... 2. Endomorphin 1/2 . these are 6 peptides long with an amino at one end. How the fuck do you build these things? Also, TAPP is another strong agonist of a similar makeup.

Piglet Member

[Image] posted 09-06-98 08:00 AM

[Click Here to See the Profile for Piglet] ------------------------------------------------------D342: You know anything about Clonitazine and Etonitazine 'potent u opioid receptor anonist; narcotic analgesic' Merck12th edition No3929. I can't find anything about this unique class of opiod analgesic. Ideas: 1. Ever checked out the structure of diphenhydramine, common antihistamine. If you cleave the ether, you end up with to very good building blocks for methadone type analgesics, I should think. 2. Ever checked out Loperamides structure. It's got the meperidine skeleton right inside and I think the amide is fine (similar to the one in dextromoramide) and although it lacks a methyl side-chain, other powerful drugs are the same (piritamide, diphenoxyl butyrate,benzitramide) and although it has a bulky group of the benzyl group (like piritimide and benzitrimide again, as well as difenoxin) it SHOULD still have quite some activity. I guess that the alcohol prevents it crossing the blood-brain barrier and the Cl makes it bind to k receptors more (just like haloperidol). a. Make ether from alcohol (protection). b. Grignard off the Cl. The amide SHOULD stay put, if you remember our discussion of some months ago... 3. Cocaine analogues. I notice in the RBI lots of 4-halo cocaine derivitives which although not scheduled, are marked as 'NO telephone orders taken for this compound, NOT for sale in europe'. a. Make para-halo benzoic acid via sandmayer procedure (swap the Cl by adding KI or KBr) or the Gatterman synthesis using butyl nitrate and CuX2 which MIGHT be better. b. DIY some acetic anhydride and make the substituted benzoic anhydride from it. c. Buy some coke, clean and degrade to ecgonine. d. Make coke analogue with i) bubble HCl gas through methanol solution of ecgonine. ii) Add benzoic anhydride. See BER 89,679(1956) or simpler still, PC by MVS Page 142. Of course, you need sodium flouroborate or HF to make the flouro-. I'm not too keen on messing with them!

All the best, Piglet :) Piglet Member

[Image] posted 09-06-98 08:05 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------PS the PABA (Para Amino Benzoic Acid) is another diet supplement which at my hippy shop is 2 shelves below the B1 ;) I'm gonna drive you crazy with mad precursor ideas! I reckon if I throw enough at you, something will stick! Mostly it's vitamins right now.

A N Onymous Junior Member

[Image] posted 09-14-98 04:11 AM [Click Here to See the Profile for A N Onymous] ------------------------------------------------------Drone342 I noticed that you and Piglet discussing the Benzimidazoles & wondered if a little bit of information might help you both. I have seen on the shelves of a US photographic supply outlet the sale of '5-Nitro Benzimidazole Nitrate' which I wondered if it might useful for you to know. It cost $95 for 100g which seems pretty cheap if you asked me. If/When I get more information I will post. I use my friend's computer so it takes me time to reply.

Piglet Member

[Image] posted 09-14-98 04:33 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------D342: Direct yourself to US Patent 5,262,428 which is a pretty cool thing about the coke analogues. I found this whilst hunting for the term 'Mazindol' which is a diet drug. I still can't find any details except for it affects the dopamine pathway in a similar manner... Piglet [Image] PS: AN: Got any synth references. I can't find out if it's useful until I know how the stuff is made!

guesswork Member

[Image] posted 11-23-98 06:29 PM [Click Here to See the Profile for guesswork] ------------------------------------------------------Hey kids. Nobody has posted here in a while, but I used to know lots about fentanyl derivatives, so I figured I'd shout in. 3-methyl-fentanyl and alpha-methyl-fentanyl are the most powerful and are relatively equally powerful. In terms of dose equivalents, they are much more soluable than heroin at room temperature.

But to those of you who haven't heard of fentanyl derivatives before, don't think drone discovered something new. They've been around since the early 80's. When they first came out people were OD'ing but no forensic lab in the nation could detect the fantastically low doses of these fentanyls it takes to kill you. There was only 1 lab in the world then that was high tech enough to sniff out 3-methyl-fentanyl overdose levels. Some Dow(?) chemist was arrested in 85(?) for trying to sell one ounce of the better n-methyl-fentanyl. His asking price was 1/2 million. At the time that much heroin equivalent was worth $13 million. But I seriously wouldn't even dream about making a drug whose overdose rate is 1/2 a grain of sand. Careful now. beagle_boy Member

[Image] posted 11-23-98 08:27 PM [Click Here to See the Profile for beagle_boy] ------------------------------------------------------I'm a little late getting in on this conversation, but in rereading this excellent thread I have a few comments. Regarding the talk of succindialdehyde, it would be best to avoid it altogether and use the succindialdehyde equivalent 2,5-dimethoxytetrahydrofuran, which is avail. OTC from photo supply places BTW. Or even better go through the nitrone route to cocaine. Are you aware of this route? Piglet: I'm not sure what turned up on your search for Mazindol info, but I'm pretty sure that it doesn't have any fun potential. It is interesting that this cpd that is a decent dopamine uptake inhibitor and still isn't worthwhile. I've always been amazed that fentanyl doesn't turn up more on the street considering how phenominally easy these analogs are to make. Maybe its the complications with dilution.

Piglet Member

[Image] posted 11-24-98 04:06 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------guesswork: Firstly, they are NOT the most powerful fentanyl derivitives by a factor of about 30. Carfentanil, Lofentanyl, remifentanyl and a HOST of others. 3-methyl is 125x morphine, carfentanil is 4000x morphine. Get the picture? One oz of 3-methyl equates to 1.1Kg smack. Even at street prices thats only about �90000. Bulk, it's about �45000. Drone never say's it's a new drug,although it IS an analoguge. The point is a more OTC synthesis. We can

ALL read the patents. Doesn't mean we can actually make it? By the way, what is N-methyl fentanyl supposed to be? If either of the 2 nitrogen's has a methyl group, it isn't a fentanyl. Unless I'm missing something? Beagle_boy: well, Mazindol IS controlled and it's structure IS a rigid-body-PEA? That Cl might be removed to make something good? Piglet [Image] beagle_boy Member

[Image] posted 11-24-98 08:41 AM [Click Here to See the Profile for beagle_boy] ------------------------------------------------------I don't see Mazindol as being worthwhile in and of itself or as a starting material. It is curious that it is a CS. I've seen a study where monkeys were trained to shoot up speed and when the speed was replaced w/ mazindol the monkeys got really pissed off and said that mazindol has no abuse potential and is no fun at all (OK, so I'm paraphrasing what the monkeys said). I guess that the DEA wants any appetite supressant to be a CS whether it has abuse potential or not. Witness the recent classification of "Meridea", another diet aid that supposedly has little to no abuse potential. But are you saying that Mazindol is a CS in UK? I wonder if independant studies of abuse potential were done.

Piglet Member

[Image] posted 11-24-98 09:12 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------Yes, it is controlled, and as I said, that chlorine group needs lopping off in my opinion. Without that I reckon it would be pretty active. How to make it, though?

beagle_boy Member

Piglet Member

[Image] posted 11-24-98 10:47 AM [Click Here to See the Profile for beagle_boy] ------------------------------------------------------Why do you reckon that it would be any more active w/o the Cl? This cpd acts in a different manner than amphet. Attempts to extrapolate SAR info from 1 class to the other are useless IMHO. [Image] posted 11-24-98 10:52 AM [Click Here to See the Profile for Piglet] ------------------------------------------------------Different manner of action? Pray tell?

beagle_boy

[Image] posted 11-24-98 11:12 AM

Member [Click Here to See the Profile for beagle_boy] ------------------------------------------------------Mazindol interacts with the dopamine transporter receptor at a site different from cocaine or BTCP, blocking reuptake. Amphetamine also inhibits the reuptake of amphetamine by interaction at another dopamine receptor site but probably more importantly it acts as an indirect DA agonist by stimulating the release of dopamine. beagle_boy Member

[Image] posted 11-24-98 11:13 AM [Click Here to See the Profile for beagle_boy] ------------------------------------------------------Whoops, typo. That should be "Amphetamine also inhibits the reuptake of dopamine...."

drone 342 Member

[Image] posted 11-24-98 05:26 PM [Click Here to See the Profile for drone 342] ------------------------------------------------------I got bad news. The reason you haven't seen a FAQ yet on tropinone-derived fentanyls is that the reaction with tropinone doesn't yield well (bad, bad yeilds (5-10%), but a product none-the-less.) Still, by using commercially available methylpiperidone instead, this method works well. Sadly, its not 100% OTC. -drone #342

Kaff Member

[Image] posted 11-30-98 12:44 AM [Click Here to See the Profile for Kaff] ------------------------------------------------------What's wrong with a yield of 5-10% on a product that's at least 100 times stronger than heroin? An FAQ would still be good just for the interesting read.

Kaff Member

[Image] posted 11-30-98 03:43 AM [Click Here to See the Profile for Kaff] ------------------------------------------------------TEST after I put on a post on this thread and returned to the Chem Discourse board and clicked on this topic (a gift from drone to dea) only the first 10 posts of it showed up. I kept clicking back and forth but didn't get the whole thread, but when I clicked on "post reply" I did get the whole thread.

Free Radical Member

[Image] posted 03-28-99 07:49 PM

Slappy

[Image] posted 04-04-99 06:32 AM

[Click Here to See the Profile for Free Radical] ------------------------------------------------------I guess you can still post here. If anybee can find this thread within a thread.

Member [Click Here to See the Profile for Slappy] ------------------------------------------------------DroneWhat is the status of that paper? Are you still working on it, or have you given up all together? -S PS- Take a look at the photosynthesis thread on the novel forum. niteflier Member

[Image] posted 04-04-99 03:42 PM [Click Here to See the Profile for niteflier] ------------------------------------------------------Drone...how is this going??? While not personally interested in these compounds I share your conviction that this info should be very public. Publishing is an exellent idea... I would help in the publishing part any way I could...It would change the world as we know it...

- - - - Drone, you are a hero to any hard-core opioid aficionado! Hey, everybody! DopaMan here. Sorry for just suddenly contributing here out of the blue, but I know a lot about fentanyls, and have had personal experience. I must disagree with the potencies listed before. Remifentanil, which is new on the market as an anesthetic/analgesic, like alfentanil, is only about half, to one-fourth, as potent as fentanyl, depending on the patient and the circumstances of use. It is approximately equivalent in potency to alfentanil. This information was furnished from the 1998 PDR, as well as other sources. Next, fentanyl is approximately 100 to 150 times as potent as morphine, some say 80, some say 200. I say 100-150 times as potent. I, personally, have had fentanyl five times, for a total of 10 injections. I have never been so high as the first time they gave me fentanyl. Indeed, it produces the most euphoria of any opioid, or drug, for that matter, that I have ever had. Much more so than morphine, and the rush, though it takes longer by about twenty seconds, to hit you than morphine, is sublime. Hence, Sublimaze! II never had any breathing trouble, and I was given nearly anesthetic doses on a few occaisions (one time as high as 0.2 mg, as the normal dose is about 0.025-0.05 mg. I did pass out when they gave me propofol on top of that and the Versed (midazolam HCl), but only because of that damn propofol! I think that breathing trouble must have been a unique, idiosyncratic reaction, as it's called. Something unusual, and unique to IceKat, or to a small group of the population. Also, nausea is unusual for fentanyl, although itching is a constant for all opioids. I had a bit of a problem with that when I first had fentanyl. I don't think the therapeutic ratio of fentanyl is actually that much higher than H, but I could be wrong. They can use it as an anesthetic by itself, with oxygen, which they sometimes do for delicate triple bypass, and other open heart procedures, which they certainly

couldn't do with heroin, but they dosage is crucial, with higher concentrations, and naloxone must be onhand. By the way, there are no bad effects from being administered naloxone by itself. Check the PDR. One can be given nearly 1000 times the normal dose with only a sense of malaise resulting. It would, of course, make it awful for someone in pain, as they would need their endorphins to work, which it would block effectively, but, otherwise, it's pretty-well-tolerated shit, unless you happen to be opioid-dependant, in which case you would spontaneously withdraw. I'm not sure where a person would get the idea it is somehow a nasty substance, aside from the fact that it'll ruin your high. Next, sufentanil-I've never had sufentanil, but I know, once again from a PDR (1994), that it's 7-10x more potent than fentanyl (so, about 1000 x morphine, give or take). I happen to know that TMF, or 3-methylfentanyl, used as either the hydrochloride or isothiocyanate, is about 5,500 x as potent as morphine, compared to the 2000-3000 times morphine potency of AMF, or alpha-methylfentanyl hydrochloride. It is not only 150 times as potent as morphine--that's fentanyl's potency. The reason people make TMF, or did so much in the eighties, is it affords much, much greater potency over original fentanyl. I have read experimental anesthesiology books, and have this on good authority. Lofentanil is about 4000-8000 times as powerful as morphine, second only to its predecessor, carfentanil, the ultimate opioid. This seems strange to me, as it is the 3-methyl, levorotatory analogue of carfentanil, so it seems like it should be more potent. I guess these rules are sometimes wacked. Carfentanil is one of the two most potent drugs ever conceived. I checked this one out in a vet's reference, as it is used now in place of etorphine HCl, in a liquid for darts called Wildinil. According to the reference, and a few other books I've looked in, it has a clinical potency of 10,000 times that of morphine; yes, seriously. I have it on good authority that this is the case. Check it out. It's true. It may actually be the most potent drug on the planet. It is considered to be an exceptionally powerful, euphoric, mu agonist opioid of the morphine/fentanyl type, but it is so potent that it kills at smaller doses than anything else in the known world. For example, it is more lethal to spill the solution on you're skin, or inhale it, than VX, for fuck's sake! It, or this one other opioid with a long numeric name starting with the letters and numbers Ro-18...something, I can't remember which, was listed in the Guinness Book of World Records, about ten years back, when they actually had a more extensive range, and a drug/chemical extremes section, as the most lethal substance on earth, due to its extreme potency. It and carfentanil are one in the same, I understand. They are both at least 10,000 times morphine potency. A shoe box full of the stuff would supply the entire double continent of North/South America with narcotizing doses of an opioid every day for months! Imagine making a key-low (aka kilo) of the stuff. You would be set for 10 lifetimes, as long as you had good distributors, and as long as you weren't propositioning African-American employee's, like at DuPont, where that one entrepreneuring chemist who made all that TMF, tried propositioning the janitor, because of ridiculous stereotype beliefs that black guys are automatically hooked up. I would personally love to here more about the making of fentanyl analogues from phenylpropanolamine, and what the chemical designation of that one from tropane would be. Lastly, that 5'-nitrobenzimidazole is something to definitely take a look at! It could be used to make either etonitazene or clonitazene! Both are about 1500 times as potent as morphine! Etonitazene mesylate is chemically identified as

1-(beta-diethylaminoethyl)-2-para-ethoxybenzyl-5'-nitrobenzimidazole methane sulphonate. Clonitazene is the 2-para-chlorobenzyl- analogue. They are extremely potent. The most so of any open-chain opioids, to my knowledge. I will post again after I research these compounds a bit more, or even before then, as I have a few developing synthesis ideas myself. Take it easy everybody! The high-binding-affinity superhero you know as DopaMan : ) !