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Umfrage: Ist Synthetisches Kokain eine Alternative?
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Diskussion: Kokain Synthese

Allgemein gibt es ja viele Stoffe, dir versuchen, ein wenig das Kokain nachzuahmen bzw. ähnliche Wikungen erziehlen.
Nun ist aber das Kokain immernoch unvergleichbar.
Was sagt ihr, wäre ein komplett synthetisches Kokain eine realistische Alternative? Kosten, sowie Wirkungstechnisch? (Auch Nebenwirkungsmäßig z.B. stärkere/schwächere Abhängigkeit und Auswirkungen auf Körper und Geist.
Wie würdet ihr es anstellen? Oder habt ihr es schon probiert?

Ich persönlich kenne kaum eine Droge, die man zu 100% so wie das Original hinbekommen hat. Wirkungs wie Geschmakstechnisch.

Wie soll bitte vollsynthetisches Kokain eine andere Wirkung haben als biosynthetisch hergestelltes? Wenn beides als Reinstoff vorliegt kann der Körper keinen Unterschied feststellen, wie denn auch?
Scheiß auf Recht und Ordnung, Einigkeit und Freiheit,
Scheiß auf scheiß Kulturen aus der scheiß Steinzeit!

Ich glaube dem Rit4lin geht es um RCs, die nahe an Kokain herankommen sollen. Trotzdem finde ich die Umfrage ziemlich seltsam, da Drogenwirkungen zwangsläufig ziemlich subjektiv sind - abgesehen davon kann man wohl kaum abschätzen, welche weiteren Derivate wohl noch erforscht werden und welche Wirkungen und Nebenwirkungen diese dann haben.
"I had originally called this family the "natural" amphetamines, but my son suggested calling them the "essential" amphetamines, and I like that."

Schau dir mal das hier an @Ritalin

Also stelle mir diese Alternative schon ziemlich interessant vor

Kann man schon machen, ist aber äusserst aufwändig:

Acetonedicarbonylic Acid Anhydride

To a solution of 30 ml glacial acetic acid and 22 ml of acetic anhydride (Fisher) at 10°C was slowly
added 20g (0.684 mol) of 1,3-acetonedicarboxylic acid (Aldrich). The temperature was not allowed
to rise above +12°C until the reaction was complete. For runs where precipitation of product hadnot
occurred within 3 h, it was induced by the addition of benzene. The product was filtered by suction
filtration, washed with 100 ml of glacial acetic acid, and next washed with 100 ml of benzene. It
was allowed to dry yielding 14.8 g of white powder (84%).


This can be purchased, too. 23.2 g of succinaldoxime powder in 410 ml of 1 N sulfuric acid and add
dropwise with stirring at 0°C a solution of 27.6 g of sodium nitrite in 250 ml of water over 3 hours.
After the addition, stir and let the mixture rise to room temp for about 2 hours, taking care not to let
outside air into the reaction. Stir in 5 g of Ba carbonate and filter. Extract the filtrate with ether and
dry, evaporate in vacuo to get the succindialdehyde. This was taken from JOC, 22, 1390 (1957). To
make succinaldoxime, see JOC, 21, 644 (1956).

In a 2 liter 3 necked flask equipped with a stirrer, reflux condenser, and an addition funnel, is mixed1
liter of ethanol, 67 g of freshly distilled pyrrole, and 141 g of hydroxylamine hydrochloride. Heat
to reflux until dissolved, add 106 g of anhydrous sodium carbonate in small portions as fast as
reaction will allow. Reflux for 24 hours and filter the mixture. Evaporate the filtrate to dryness
under vacuo. Take up the residue in the minimum amount of boiling water, decolorize with carbon,
filter and allow to recrystallize in refrigerator. Filter to get product and concentrate to get additional
crop. Yield of succinaldoxime powder is a little over 40 g, mp is 171-172°C. 5.8 g of the above
powder is placed in a beaker of 250 ml capacity and 54 ml of 10% sulfuric acid is added. Cool to
0°C and add in small portions of 7 g of sodium nitrite (if you add the nitrite too fast, nitrogen
dioxide fumes will evolve). After the dioxime is completely dissolved, allow the solution to warm
to 20°C and effervescence to go to completion. Neutralize the yellow solution to litmus by adding
small portions of barium carbonate. Filter off the barium sulfate that precipitates. The filtrate is 90%
pure succindialdehyde and is not purified further for the reaction to create tropinone. Do this
procedure 3 more times to get the proper amount for the next step, or multiply the amounts given by
four and proceed as described above. Take the total amount of succinaldehyde (obtained from 4 of
the above syntheses combined) and without further treatment or purification (this had better be 15.5
g   of   succindialdehyde)   put   into   an   Erlenmeyer   flask   of   4-5   liters   capacity.  Add   21.6   g   of
methylamine hydrochloride, 46.7 g of acetonedicarboxylic acid, and enough water to make a total
volume of 2 liters. Adjust the pH to 8- 10 by slowly adding a saturated solution of disodium
phosphate. The condensate of this reaction (allow to set for about 6 days) is extracted with ether, the
ethereal solution is dried over sodium sulphate and distilled, the product coming over at 113°C at 25
mm of  pressure is  collected.  Upon  cooling,   14  g  of  tropinone  crystallizes  in   the pure  state.
Tropinone can also be obtained by oxidation of tropine with potassium dichromate, but I could not
find the specifics for this operation.


10 g of pyrrolidinediethyl diacetate are heated with 10 g of cymene and 2 g of sodium powder, the
reaction taking place at about 160°C. During the reaction (which is complete in about 10 min) the
temp should not exceed 172°C. The resulting reaction product is dissolved in water, then saturated
with potassium carbonate, and the oil, which separates, is boiled with dilute sulfuric acid. 2.9 g of
tropinone picrate forms and is filtered. Here are two more formulas devised by Willstatter that
produce tropinone from tropine. Take note of the yield differences. To a solution of 25 g tropine,
dissolved in 10 times its weight of 20% sulfuric acid are added 25 g of a 4% solution of potassium
permanganate in 2 or 3 g portions over 45 min while keeping the temp at 10-12°C. The addition of
permanganate will cause heat (keep the temp 10-12°C) and precipitation of manganese dioxide. The
reaction mixture is complete in I hour. A large excess of NaOH is added and the reaction is steam
distilled until I liter of distillate has been collected. The tropinone is isolated as the dibenzal
compound by mixing the distillate with 40 g of benzaldehyde in 500 cc of alcohol and 40 g of 10%
sodium hydroxide solution. Let stand several days to get dibenzaltropinone as yellow needles.
Yield: 15.5 g, 28%. Recrystallize from ethanol to purify. A solution of 12 g of chromic acid in the
same amount of water (12 g) and 60 g of glacial acetic acid is added dropwise with stirring over a
period of 4 hours to a solution of 25 g of tropine in 500 mL of glacial acetic acid that has been
warmed to 60-70°C and is maintained at this temp during the addition. Heat the mixture for a short
time on a steam bath until all the chromic acid has disappeared, cool and make strongly alkaline
with NaOH. Extract with six 500 mL portions of ether and evaporate the ether in vacuo to get an oil
that crystallizes readily. Purify by converting to the picrate or fractionally distill, collecting the
fraction at 224-225°C at 714 mm vacuo. The tropinones can be used in the above formula (or in a
formula that you have found elsewhere) to be converted to cocaine. Remember to recrystallize the
2-carbomethoxytropinone before converting to methylecgonine.


A mixture of 1.35 g of sodium methoxide (this is sodium in a minimum amount of methanol), 3.5 g
of tropinone, 4 ml of dimethylcarbonate and 10 ml of toluene is refluxed for 30 min. Cool to 0°C
and add 15 ml of water that contains 2.5 g of ammonium chloride. Extract the solution after shaking
with four 50 ml portions of chloroform, dry, evaporate the chloroform in vacuo. Dissolve the oil
residue in 100 ml of ether, wash twice with a mixture of 6 ml of saturated potassium carbonate and
three ml of 3 N KOH. Dry and evaporate in vacuo to recover the unreacted tropinone. Take up the
oil in a solution of aqueous ammonium chloride and extract with chloroform, dry, and evaporate in
vacuo to get an oil. The oil is dissolved in hot acetone, cool, and scratch inside of flask with glass
rod to precipitate 2-carbomethoxytropinone. Recrystallize 16 g of this product in 30 ml of hot
methyl acetate and add 4 ml of cold water and 4 ml of acetone. Put in freezer for 2.5-3 hours. Filter
and wash the precipitate with cold methyl acetate to get pure product.

Six liters of 4.4 pH citrate buffer was made by diluting 35.3 g of citric acid and 38.8 g of sodium
citrate   dihydrate   to   volume.   To   the   buffer   was   added   32.0   g   (0.48   mol)   of   methylamine
hydrochloride (Fisher) and 12.8g (0.32 mol) of sodium hydroxide. The succindialdehyde solution
was added dropwise to the buffer over 10 min with stirring at room temperature. The mono-methyl
ester solution was next added dropwise over 10 min with stirring. The reaction was stirred 48 h at
room temperature. The reaction was extracted in 250-ml portions by making the pH 12 with
concentrated ammonium hydroxide and extracted 4 times with 200 ml of chloroform. The extracts
were dried over sodium sulfate and evaporated in vacuo. The resulting yellow oil was dissolved in
200 ml of dry diethyl ether and filtered. The filtrate was evaporated in vacuo. The oil was next
dissolved into 200 ml of petroleum ether and filtered. The filtrate was evaporated in vacuo and the
resulting oil was allowed to hydrate upon standing. The crude hydrate was 95% pure and purified
further by sublimation to yield snow white flakes, mp 96-98.5°C. Yield: 58.9 g (86%).

To a solution of 26.60 g (0.124 mol) of sublimed racemic 2-CMT in 106 ml of absolute ethanol was
added dropwise a solution of 18.57 g (0.124 mol) of (-)-tartaric acid in 133 ml of absolute ethanol.
After 48 h the mother liquor was decanted and set aside. The crystals were washed with 50 ml of
absolute ethanol and then dissolved into a minimal amount (approx. 200 ml) of hot dry methanol.
The solution was filtered while hot into an Erlenmeyer flask and covered. The solution was left
undisturbed for 72 h. The solution was decanted off and combined with the first mother liquor. The
crystals of anhydrous (-)-2-CMT bitartrate were washed with 100 ml of dry acetone and dried
yielding 6.8g (30%), [α]D 24 -16.9° (c=2, H2O). Findlay18 reported [α]D 20 -16.9° (c=2, H2O).
The mother liquors were evaporated to dryness and dissolved into 200 ml of water, made pH 8 with
sodium carbonate, and extracted 5 times with 200 ml of methylene chloride. The extracts were dried
over sodium sulfate and evaporated in vacuo. The (+)-enriched 2-CMT was hydrated yielding 17.5
g of powder.

To a solution of 17.2 g (0.08 mol) of (+)-enriched 2-CMT in 70 ml of absolute ethanol
was added a solution of 12.0 g (0.08 mol) of (+)-tartaric acid in 86 ml of absolute ethanol.
Subsequent recrystallizations yielded 6.95 g of anhydrous (+)-2-CMT bitartrate (30%), [α]D 24
+16.9° (c=2, H2O). Freebasing the mother liquors and retreatment with (-)-tartaric acid yielded 6.0
g more anhydrous (-)-2-CMT bitartrate, [α]D 24 -17.0° (c=2, H2O). Thus the overall yield of
anhydrous (-)-2-CMT bitartrate was 12.8 g (57%).


0.4 mole of tropinone is suspended in 80 ml of ethanol in a Parr hydrogenation flask (or something
that can take 100 psi and not react with the reaction, like stainless steel or glass). 10 g of Raney
Nickle is added with good agitation (stirring or shaking) followed by 2-3 ml of 20% NaOH
solution. Seal vessel, introduce 50 psi of hydrogen atmosphere (after flushing vessel with hydrogen)
and heat to 40-50°C. After no more uptake of hydrogen (pressure gauge will hold steady after
dropping to its lowest point) bleed off pressure and filter the nickle off, rinse out bottle with
chloroform and use this rinse to rinse off the nickle while still on the filter paper. Make the filtratebasic
with KOH after cooling to 10°C. Extract with chloroform dry, and evaporate the chloroform
in vacuo to get an oil. Mix the oil plus any precipitate with an equal volume of dry ether and filter.
Add more dry ether to the filtrate until no more precipitate forms, filter and add to the rest of the
precipitate. Recrystallize from isopropanol to get pure methylecgonine. Test for activity. If active,
skip down to the step for cocaine. If not active, proceed as follows. Stir with activated carbon for 30
min, filter, evaporate in vacuo, dissolve the brown liquid in methanol, and neutralize with 10% HCl
acid in dry ether. Evaporate the ether until the two layers disappear, and allow to stand for 2 hours at
0°C to precipitate the title product. There are many ways to reduce 2-carbomethoxytropinone to
methylecgonine.  I chose  to  design a Raney Nickle reduction  because it is  cheap  and  not  as
suspicious as LAH and it is much easier than zinc or sodium amalgams.

Into a three-neck 500 ml round bottom flask was placed 7.70 g (0.036 mol) of (-)-2-CMT hydrate
with 51 ml of ice cold 10% sulfuric acid. Bromophenol blue (approx. 2 mg) indicator was added.
With stirring the solution was treated with 1028 g of 1.5% sodium amalgam in small portions over
2.5 h. The temperature was kept under +5°C. The pH was monitored via the indicator and kept
between pH 3 and 4 with cold 30% sulfuric acid. Periodic addition of water was necessary to
dissolve sodium sulfate salts. The reaction was stirred an additional 45 min after the addition of
amalgam was complete. The solution was separated from the mercury, adjusted to pH 12 with
sodium hydroxide and extracted three times with 200 ml of chloroform. The extracts were dried
over sodium sulfate and evaporated in vacuo to a light green oil containing a 3:1 ratio of EME to
PEME. The  oil  was   dissolved   into   200   ml  of   petroleum  ether   and   filtered.  The  filtrate  was
evaporated in vacuo. The resulting oil was dissolved into 500 ml of dry diethyl ether and the
hydrochloride salts were made with ethereal HCl. The salts were filtered and immediately dissolved
into a minimal amount of dry methanol. The methanol was evaporated in vacuo and 120 ml of dry
chloroform was added to the crystals. The slurry of crystals was filtered and dried yielding 2.28 g of
(+)-ecgonine methyl ester hydrochloride (27%). The product was recrystallized from methanol and
diethyl ether to yield 2.2 g of pure product [α]D 24 +52.3° c=1, MeOH), mp 213-214°C.


4.15 g of methylecgonine and 5.7 g of benzoic anhydride in 150 ml of dry benzene are gently
refluxed for 4 hours taking precaution against H2O in the air (drying tube). Cool in an ice bath,
acidify carefully with hydrochloric acid, dry, and evaporate in a vacuum to get a red oil which is
treated with a little portion of isopropanoi to precipitate cocaine. As you can see, this is quite a
chore. The coca leaves give ecgonine, which as you can see, is only a jump away from cocaine. If
you can get egconine, then dissolve 8.5 g of it in 100 ml of ethanol and pass (bubble) dry HCl gas
through this solution for 30 min. Let cool to room temp and let stand for another 1.5 hours. Gently
reflux for 30 min and evaporate in vacuo. Basify the residue oil with NaOH and filter to get 8.4 g of
methylecgonine, which is converted to cocaine as in the cocaine step above. Below is given a
somewhat easier method of producing tropinone by the general methods of Willstatter, who was
instrumental in the first synthetic production of cocaine and several other alkaloids. After reviewing
this method, I found it to be simpler than the above in many respects.  In an oven-dried 100-ml
round bottom flask was added 1.00g (4.25 mmol) of (+)-ecgonine methyl ester HCl with 7 ml of dry
pyridine and stirred in an ice bath. The reaction was protected from moisture with argon. Dropwise
over 5 min was added a solution of 0.8 ml (6.85 mmol) of benzoyl chloride in 5 ml of pyridine.
After addition was complete the ice bath was removed and the reaction was stirred 24 h under
argon. Dry acetone (200 ml) was added and the slurry was filtered by suction filtration. The crude
(+)-cocaine hydrochloride was washed with an additional 100 ml of dry acetone. The product was
dried yielding 1.28 g (89%). The hydrochloride was dissolved into 20 ml of water, made pH 8 with
5% ammonium hydroxide, and extracted 4 times with 50 ml of methylene chloride. The solvent was
dried over sodium sulfate and evaporated in vacuo. The free base was recrystallized from diethyl
ether and petroleum ether yielding 1.01 g (78%) of pure (+)-cocaine base.

man könnte arecolin mit benzoesäureanhydrid reagieren lassen wie bei dem letzten schritt wie von dir beschrieben. (arecolin synthese aus vitamin B3) - man kann natürlich auch alles Methanol mit Ethanol und ethylbromid substituieren - das wäre ein cocain analog der auch wirksam wäre ^^ mit arecolin auch aber ethanol is halt einfach beschaffbar und ich meine das ethylcocain potenter seien soll als sein Vater - deshalb ist es doch ein versuch wert Big Grin

Mir ging es um synthetische alternativen.
Sprich eir reden davon, einen synthetischen stoff zu produzieren der wirkt wie koks aber es nicht ist
entschuldigt die zugegebenerweise beschissene ausdrucksweise

Weiß hier jemand eigentlich was zum genauen Rechtsstatus von Arecolin? Ich finde dazu nicht wirklich was, meine aber Mal gehört zu haben, dass die Salze verschreibungspflichtig sind (keine Ahnung ob das stimmt)

Würde mich freuen wenn mich da jemand aufklären könnte

nunja du könntest betelnüsse kaufen, und das arecolin extrahieren - ist aber mühsam - dann lieber selber synthetisieren.

wer das vor hat und nicht an NaBH4 kommt sollte den thread auf siencemadness ganz genau durchlesen..

Wenn ihr an dem Thema auch so interressiert seit.
Ich hab nen Thread zur Vollsynthese schon vor ner weile gestartet. Hängt aber derzeit noch an der Informationsbeschaffung.
Ne Brauchbare deutsche Anleitung ist schon da.
Würd mich sehr freuen wenn ihr euch beteiligt.
Die Infos dazu sind ja stark gestreut im ganzen netzt, vieleicht schaffen wirs gemeinsam sie dort etwas zusammenzuführen.
Ziel soll eine zusammenhängende Anleitung mit praxistipps sein so wie es gefühlte 1000 für Amphe gibt.
Ich komm nur langsam vorran alleine, zumal ich jeden scheiß nachschlagen muss weil ich kein Chemiker bin.
Danke schonmal
Die guten Dinge kommen zu denen, die warten können. Thumbupleft
Si Vis Pacem Para Bellum.

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