Welcome to the complete guide of how to make cocaine. If you do

everything right you are going to be king of the world, either in your

own world or in the real world. Please read the disclaimer at the end of

this text.

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The basic formula for cocaine starts by purchasing or making tropinine,

converting the tropinone into 2-carbomethoxytropinone (also known as

methyl-tropan-3-one-2-carboxylate), reducing this to ecgonine,

and changing that to cocaine.

Succindialdehyde. 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* 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 t

aken from JOC, 22, 1390 (1957). To make succinaldoxime, see JOC, 21,

644 (1956).

Complete Synthesis of Succindialdehyde. JACS, 68, 1608 (1946). In a 2 liter

3 necked flask equipped with a stirrer, reflux condenser, and an addition

funnel, is mixed 1 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*.

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* 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* 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* at

25 mm of pressure is collected. Upon cooling, 14 g of tropinone

crystallizes in the pure state.

2-Carbomethoxytropinone. 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* and add 15 ml of water that contains 2.5 g of ammonium chloride.

Extract the solution after shaking with with four 50 ml portions of...