UPDATED:: MAY 22 '13

I have figured out it is pointless to do this with mdma as is, aziridines.. ehh.. this as is needs a new revamp.. my new research intrests focus on reduction of phenylalanine to the corresponding alcohol via various reductions and then performing the wenker or mitsonubu reactions and forming amphetamine. Then via formylation via formic acid, the amide will be reduced by nabh4 and voila,

meth

however i have had another dream that involved dakin west reaction of phenylalanine, causing subsequent formylation resulting in the amide, and the aldehyde

however there is issues with this as formic anhydride is not available and must be generated in situ via 2 ACO and 1 COOH equiv. however


if you formylate the amine first, then perform dakin west, you receive an aldehyde from the carboxyllic acid reduction(the amine CANNOT form more than one formic addition to itself, the geometry is VERY UNFAVORABLE, it can only readily form, FORMAMIDE)!!!!!

now you have N-(1-oxo-3-phenylpropan-2-yl)formamide or N-(1-formyl-2-phenylethyl)formamide

http://www.chemsink.com/compound/21615338/

subsequent reduction with borohydride leads you to methamphetamine, racemic, providing DL-phenylalanine was used (sorry no reversal in the optical resolution)

my dream is only possible with others attempts too..






****OLD:::_________________________-
In my recent findings I have realized an excellent method to prepare mdma from various legal chems in an offbeat way..

PART A
Catechol+DCM-----> BENZODIOXOLE

BENZODIOXOLE +NBS(or other electrophillic bromine agent) ----> Bromo Benzodioxole

PART B

n-methylalanine ---> Reduction to 2-(methylamino)-1-propanol
2-(methylamino)-1-propanol or 1-(methylamino)-2-propanol + P-sulfonyl chloride(tosyl chloride) ---> tosyl aziridine

http://lego.chemistry.tripod.com/pea/tosylaziridine.html

tosyl aziridine+ Bromo Benzodioxole ---->  N-[1-(2H-1,3-benzodioxol-5-yl)propan-2-yl]-4-methylbenzene-1-n-methylsulfonamide 

N-[1-(2H-1,3-benzodioxol-5-yl)propan-2-yl]-4-methylbenzene-1-n-methylsulfonamide  +  (H+) ------> MDMA .




ALL FROM CATECHOL, however the formation of n-methyl alanine is troublesome and tosyl aziridines;NBS may be hard for some to source. but I am undergoing attempting this method very shortly. Hopefully my thoughts are not insane.

PICS ATTACHED OF TOSYL AZIRIDINE (unmethylated, n-methyl alanine will lead to MDMA, the former, MDA)

http://www.orgsyn.org/orgsyn/orgsyn/prepContent.asp?prep=cv1p0021
http://www.orgsyn.org/orgsyn/orgsyn/prepContent.asp?prep=cv8p0119
http://www.sciencemadness.org/talk/viewthread.php?tid=16065
http://www.sciencemadness.org/talk/viewthread.php?tid=16129



thiophenechemistry

L-alaninol is not a common body building supplement, l-alanine is. If you want the alcohol you are going to have to make it so throw a reducing agent like sodium borohydride plus some other chems into the mix just to make alaninol.... Oh, you could also probably nix the methylation at the end. Although you can methylate mda to mdma no one does since the yield is so shitty.

You are completely right, and my mistake I was slightly intoxicated posting this, the compounds needed to form MDMA are

1-(Methylamino)-2-propanol

or

2-(Methylamino)-1-propanol

When the aziridine is formed it will migrate to the 2nd carbon regardless when broken to become more stable,

My thoughts were dumbfounded though as this precursor is relatively new to the industry also

other compounds i have found that could be used are
1-chloro-3-methylamino-propan-2-ol
2-methylaminopropane-1,1-diol
2-(methylamino)propionic acid (n-methyl alanine)  must be reduced to the alcohol
or 2-(methylamino) propanal
or 3-methylamino propanal

http://www.sciencemadness.org/talk/viewthread.php?tid=16065
http://www.sciencemadness.org/talk/viewthread.php?tid=16129

The issue now is n-methylalanine production, but these threads speak of it. if so then production of bromo benzodioxole, and forming the aziridine would be the hardest part to the production, besides the workup

In my recent quests I realized I was looking in the wrong direction! (and n-methyl alanine can form the aziridine, look around)

The methyl amino moeity can be present in our friend METHYLONE

Reduction of methylones' carbonyl to an alcohol , therefore methyl amino alcohol- the aziridine can be formed from this, there are synths of it working on N-Alkyl derivs and aromatic amino alcohols, the easiest way is tosylation which creates a nitrogen intermediate with 4 bonds(seemingly unstable), however the aziridine triangle's two bottom carbons are connected to a methyl, and a ring. Thus more stable, as well as the 4 substituted nitrogen is connected to a SO2 group, pulling the ring the opposite way. Stable enough to be isolated.

http://www.organic-chemistry.org/namedreactions/wenker-synthesis.shtm

Its called the wenker synthesis and it will work on the methyl amino alcohol, formerly known as MD-Ephedrine,

Think of Methylone as MD-Methcathinone, and the MD-amino alcohol as ephedrine.

A simple reduction of the carbonyl to the alcohol will allow aziridine formation-what is discussed in the link, then tosylation at room temperature with carbonate, and acetonitrile as the solvent, at room temperature occurs to form the aziridine.

The tosyl aziridine is protonated and you are left with mdma

Methylone via Reduction and Wenker's aziridine synthesis,with subsequent  protonation can lead to relatively cost-ish effective MDMA..

using azidrine... Don't like that....

This method will also work on phenylalanines carboxyllic acid functionality if it is reduced to an alcohol!

the aziridine formation wil work on any 1-ol 2-amino,  or 1-amino-2-ol, or 3-amino -2-ol as the amine migrates to the 2ndary carbon over the primary and the tertiary...

Just need to find a safe way to reduce the ketones without too low yields..

thiophenechemist

Hmm...  This is all very timely for me because I just recently saw an experiment where methylone was reduced via CTH (methylone freebase, Pd/C, formic acid, catalytic KCOOH, alcohol solvent, stirred at r.t.).  The hope was that complete hydrogenolysis of the benzylic ketone would occur.  Instead, a compound which was found to be completely inactive at a dosage of 150 mg was created.  The only product that this bee could imagine is your mentioned MD-ephedrine.  So now I suppose there is something that could be done with this inactive crap.  The route seems strange though, first reaction with sulfuric acid to form the sulphonate salt and isolation of salt, but then deprotonation to enable ring closure followed by protonation to final product?  Would you suppose to do both the deprotonation and protonation in the same pot?  Also, what solvent(s) would be ideally used for this?  Would all of this be done under reflux?


While the attempted CTH was not successful, I did find a paper that shows that it can be done via CTH.  They even optimized the reactants: "Catalytic transfer hydrogenolysis of ?-methylbenzyl alcohol using palladium catalysts and formic acid" Applied Catalysis A: General
Volume 354, Issues 1–2, 15 February 2009, Pages 38–43

This was found on the hive too

http://about.mdma.ch/000184201.html

very informative, their methods utilize gringards however..

still no mention of the methylamino alcohol forming the aziridine with tosyl chloride.. im not sure if the sulfone could help stabilize it, but even then it would be pretty reactive... im just not trying to get JUST amphetamine, or just MDA, fuck that