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From: an26424@anon.penet.fi (Badsector)
Date: Thu, 22 Jul 1993 15:20:21 GMT
Newsgroups: alt.drugs
Subject: Methcathinone Info

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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>Of course, I guess the college guy figured out that everything needed was
>right under the counter.  Now what's the government going to do?  Outlaw
>batteries and drain cleaners?  I wouldn't put it past them.

i really doubt it.

-- 
Lamont Granquist      drugz: ftp.u.washington.edu:/pub/user-supported/alt.drugs
lamontg@cs.washington.edu    personal: !finger lamontg@cs.washington.edu | more
"Conservative: n. One who admires radicals centuries after they're dead."

=============================================================================

From: cooper@hacktic.nl (cooper)
Newsgroups: alt.drugs
Subject: Re: Ephedrine Derivatives
Date: 10 Oct 1993 14:12:39 +0100
Message-ID: <2991olINNo8m@xs4all.hacktic.nl>

dyer@spdcc.com (Steve Dyer) writes:
>In article <1993Oct9.200043.25880@news.yale.edu> potter@minerva.cis.yale.edu (Philip G. Potter) wries:
>   >It is supposedly easy to make, using Ephedrine Hydrochloride (over the
>   >counter stimulant) and other household chemicals.  Do anyone have any
>   >information on this.

>You've got to be kidding.  You'd need a chemistry lab.

Well, a chemistry lab and some knowledge _might_ help, but hey, if you wanna
give it a shot, Here's howto: (well, at the end of this post, that is!
Oh this is the end huh?? Ok, here goes:

I've never tried this synthesis, and I can't be sure baout anything. However,
if your kitchen does not explode, and you have a good time anyway, lemme know.

	Methcathinone

	Preparing the ephedrine/pseudoephedrine solution: 

	  Method A: 
	    Add enough water to completely dissolve pure ephedrine or
	    pseudoephedrine. 

	  Method B: 
	    Wash sudaphed tablets in cold water until most (it's impossible
	    to get all of it) of the red coating is gone.  Put the tablets
	    in hot water, heat them to boiling, and stir until the tablets
	    have completely dissolved.  Filter off the liquid. 

	The amount of water the (pseudo-)ephedrine [I'll call it
	ephedrine from now on for simplicity] is dissolved in is not too
	important - it should be as little as possible, but at least as
	much as the amount of sulfuric acid that is added later (to
	insure to that the potassium dichromate dissolves). 
	To this aqueous mixture add 0.62 grams of potassium dichromate
	for every gram of ephedrine in the solution.  If you used
	sudaphed tablets, figure by the theoretical amount in
	solution (number of tablets X content of each tablet).  Slowly
	add 3ml Sulfuric for each gram ephedrine, stirring as you add
	it. 

	Let react for 30-60 minutes.  The color should go from a bright
	red/orange to a dark color (a mixture of green and orange from
	the two ionization states of the chromium). 
	Basify the solution with concentrated sodium hydroxide solution
	until you see the solution become a bright green (green with a
	white precipitate - the methcathinone).  This happens above pH
	8.  Try not to add too much hydroxide (if you do the solution
	becomes black and there is probably some decomposition of the
	methcathinone). 

	Extract 3-4 times with naptha (add the naptha, shake it up,
	pour off as much naptha as you can - but DON'T get ANY reaction
	mixture in the extracts!).  Use as much naptha as would equal
	about 50-100 percent of the reaction mixture. 


	Quickly add the extracts to 25ml of hydrochloric acid, diluted
	1 part 36% HCl to 4-5 parts water.  Shake the mixture, extract
	off the aqueous (lower) portion.  This is an acid solution of
	the methcathinone.  [you may want to extract a second time with
	HCl to get a slightly higher yield, a 3rd time adds nothing.]
	Evaporate the mixture under low to medium heat (preferably
	under a vacuum) until it becomes thick.  Add acetone and stir
	it a little.  if the mixture doesn't become white (crystalline)
	right away, it hasn't been evaporated enough.  Continue
	evaporating and adding acetone until it does.  Be careful not
	to burn the thick mixture (adding acetone helps keep the
	temperature down). 

	After getting crystals/precipitate, cover the mixture tightly
	and put in a freezer for 15 minutes.  Remove from the freezer,
	filter the crystals off and wash with a small amount of cold
	acetone. 
	[If the crystals are less than white, you may want to purify
	them by boiling and stirring them in acetone again, cooling
	the mixture and refiltering as described above.]

	The white crystals/powder is methcathinone HCL.  I wouldn't
	take more than 20mg for a first dose, and I wouldn't take it if
	I had a history of heart disease or stroke in the family, or if
	I had high blood pressure.  Really, really habit forming.  Very,
	very pleasurable.  BE CAREFUL.  Don't introduce this stuff to
	kids or sell it or I will personally hunt you down. 

	NOTES: 
	This synthesis is very forgiving.  Substitutions of potassium
	hydroxide for sodium hydroxide, sodium dichromate for potassium
	dichromate and similar subsitution will not have an impact.  I
	wouldn't substitute anything for the sulfuric acid, however. 
	HCl is used to make the drug salt because it is so easy to
	evaporate the excess off.  Any method of making drug salts you
	are familiar with should be satisfactory. 
	Ether works a little better than naptha, but it's more
	dangerous.  I stay away from it. 
 
 
-------------------------------------------------------------------

--Cooper
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
 
	-------------



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