Methcathinone and Ephedrone

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Methcathinone and Ephedrone

Post by Helladamnleet » Fri Aug 25, 2017 12:51 pm

Methcathinone ("Cat") / Ephedrone ("Jeff").

Initially reported as a street drug in the former USSR as ephedrone [1]. Reports of the use of "Jeff" leading to "numerous" overdose deaths were, it seems, covered up by the former Russian authorities. It has been banned in the USA after several labs were seized in Michigan. It was sold as "Cat", presumably named after the African shrub Khat (catha edulis), which contains cathinone [2]. Methcathinone is related to cathinone as methamphetamine is related to amphetamine, i.e. by N-methyl substitution.

Reliable reports of effects in humans are not known to me. A recent short letter [4] in the Journal of the American Medical Association seems to me to simply to repeat assertions made in the American popular press. In the letter, it is said that users describe "Cat" as better than cocaine and meth. "Typical" doses are described as 0.5-1g and the effects described as lasting six days.

This seems to me to be unlikely. What has been reported may well be equivalent to high dose, methamphetamine abuse on the "speed freak" pattern and is probably *not* typical.

Animal studies [2] suggest methcathinone has ED50 of 1.9uM/kg (0.39mg/kg) , when compared to cocaine's 7.6uM/kg (2.6 mg/kg). This would make it *more* potent than cocaine by six times in the rat and suggests the human figure of ten times cocaine potency in the human reported on USENET as been given on Belgium television is not unrealistic. Indeed, this would put it in the same range as methamphetamine, which it may well closely resemble.

Personal communication suggests it may well be simply equivalent to methamphetamine. The bottom line may well be that most CNS stimulants are the same, whether they be cocaine, methamphetamine, amphetamine, 4-methylaminorex or methcathinone. Differing the route of administration is likely to have more effect. Smoking or injecting such drugs leads to rapid build-up of the drug in the blood stream and an intense "rush". This route is more dangerous from a toxicologic point of view and likely to lead to compulsive use. Occasional oral use in social situations is likely to be the least harmful. Some people may find CNS stimulants psychologically addictive.

Synthesis [1]

A 2000-mL Erlenmeyer flask, equipped with a magnetic stirring bar, was charged with methylene chloride (200 mL), acetic acid (10 mL) water (100 mL), potassium permanganate (2g) and ephedrine hydrochloride (2g). The solution was stirred at room temperature for 30 min. This was followed by the addition of sufficient sodium hydrogen sulfite to reduce the precipitated manganese dioxide. The aqueous phase was made basic with 5N sodium hydroxide (NaOH) and the methylene chloride was separated. The organic layer was extracted with 0.5N sulfuric acid (H2SO4). Isolation of the acid layer followed by basification with sodium bicarbonate and extraction with methylene chloride (50 mL, three times), removed the product into the organic phase. The solvent was concentrated by rotary evaporation, followed by column chromatography through neutral alumina with methylene chloride. Solvent removal through rotary evaporation produced a colorless liquid which was disolved in hexane. Gaseous hydrochloric acid was bubbled into the hexane to precipitate the amine hydrochloride to produce a 1-g (50%) yield of 2-methylamino-1-phenylpropan-1-one hydrochloride.

Ephedrone, like methamphetamine, processes one asymmetric center. Depending upon the synthetic precursor, l-ephedrine (1R,2S) or d-pseudoephedrine (1S,2R), the product expected would be d-ephedrone (2S) or l-ephedrone (2R), respectively. However, depending on the heat of the reaction or harsh extraction conditions the enolizable ketone will result in a racemic d,l-ephedrone.

Synthesis [3]

A solution composed of 0.99g of sodium dichromate and 133g of concentrated sulfuric acid dissolved in 4.46 cc of water is added slowly with stirring to 1.65g of l-ephedrine dissolved in 4.7 cc of water and 0.55 cc of concentrated sulfuric acid at room temperature. The mixture is stirred at room temperature for an additional 4 to 6 hours and then made alkaline with sodium hydroxide soloution. the aqueous mixture is extracted with two volumes of chloroform and then with two volumes of ether. The organic extracts containing the free base of 1-a-methylaminoprophenone are combined, treated with an excess of dry hydrogen chloride and the solvents evaporated. The residual 1-a-methylaminopropiophenone hydrochloride is stirred with petroleum ether, collected and purified by dissolving in ethanol and reprecipitating with ether. m.p. 182-184 o C.

(1) Zingel, K.Y., Dovensky, W., Crossman, A. and Allen, A., "Ephedrone: 2-Methylamino-1-Phenylpropane-1-One (Jeff)," Journal of Forensic Sciences, v. 36, No.3, May 1991, pp.915-920

(2) Young, R. and R.A. Glennon. "Cocaine-Stimulus Generalization to Two New Designer Drugs: Methcathinone and 4-Methylaminorex" Pharmacol. Biochem. Behav. 45(1) 229-231, 1993

(3) Glennon, R.A., Yousif, M., Kalix, P. "Methcathinone: A new and potent amphetamine-like agent." Pharmacol. Biochem. Behav. 26:547-5451, 1987.

(3) British Patent, 768,772 (1954).

(4) Goldstone, M.S., "Cat - Methcathinone - A New Drug of Abuse" Journal of the American Medical Association v269 no 19 p2508 (letter) 1993
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