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Methcathinone and Ephedrone
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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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