Cocaine synthesis

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Although this drug is categorized as a local anesthetic, I have chosen to put it in with the hallucinogens because of the psycho- tomimetic effects that it produces. Cocaine is not a phenylethyl-amine, but it produces central nervous system arousal or stimulant effects which closely resemble those of the amphetamines, the methylenedioxyamphetamines in particular. This is due to the inhibition by cocaine of re-uptake of the norepinepherine released by the adrenergic nerve terminals, leading to an enhanced adrenergic stimulation of norepinephrine receptors. The increased sense of well-being and intense, but short lived, euphoric state produced by cocaine requires frequent administration. Cocaine does not penetrate the intact skin, but is readily absorbed from the mucus membranes, creating the need to snort it. This accounts for the ulceration of the nasal septum after cocaine has been snorted for long periods. The basic formula for cocaine starts by purchasing or making tropinone, converting the tropinone into 2-carbomethoxytropinone also known as methyl-tropanonecarboxylate , reducing this to ecgonine, and changing that to cocaine. This synthesis is certainly worth performing with the high prices that cocaine is now commanding. As usual, I will start with the precursors and intermediates leading up to the product. This can be purchased, too. 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, To make succinaldoxime, see JOC, 21, Complete Synthesis of Succindialdehyde. JACS, 68, 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 g of hydroxylamine hydrochloride. Heat to reflux until dissolved, add 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. Neutralize the yellow solution to litmus by adding small portions of barium carbonate. Filter off the barium sulfate that precipitates. 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 Adjust the pH to by slowly adding a saturated solution of disodium phosphate. 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. A mixture of 1. Extract the solution after shaking with four 50 ml portions of chloroform, dry, evaporate the chloroform in vacuo. Dissolve the oil residue in 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. Filter and wash the precipitate with cold methyl acetate to get pure product. 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. 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. If active, skip down to the step for cocaine. If not active, proceed as follows. 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. 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. Gently reflux for 30 min and evaporate in vacuo. Basify the residue oil with NaOH and filter to get 8. 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. The resulting reaction product is dissolved in water, then saturated with potassium carbonate, and the oil, which separates, is boiled with dilute sulfuric acid. Here are two more formulas devised by Willstatter that produce tropinone from tropine. Take note of the yield differences. 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. Let stand several days to get dibenzaltropinone as yellow needles. Recrystallize from ethanol to purify. 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 cc portions of ether and evaporate the ether in vacuo to get an oil that crystallizes readily. 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. The webmasters of this site do not advocate the breaking of any law. Our text files and message bases are for informational purposes only. We recommend that you contact your local law enforcement officials before undertaking any project based upon any information obtained from this or any other web site. We do not guarantee that any of the information contained on this system is correct, workable, or factual. We are not responsible for, nor do we assume any liability for, damages resulting from the use of any information on this site. Ads presented by the AdBrite Ad Network. Booze - The Legal Drug. Legal Issues of Drug Use. Rare and Exotic Drugs. To the best of our knowledge, the text on this page may be freely reproduced and distributed. If you have any questions about this, please check out our Copyright Policy. Extraction of menthol from petroleum jelly.

Cocaine synthesis

Синтез Кокаина ;)

Синтез кокаина.

Biosynthesis of cocaine