from PEA to Amp

Kj12

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Hey bbgate community,
i have question about a synthesis from Phenylethylamin to Amphetamin
is it possible to make amphetamin from phenylethylamin if you methylate the alpha place from PEA with this ingredients
Methyliod, Kaliumcarbonat, Acetonitiril, H2O, natriumsulfate, Ethylacetat and sulfuric acid

i hope my english is not too bad and you can read it
 

FENTAMAS

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No way.
There are no direct and easy methods to alkylate alpha position of PEA, i.e. construct new Carbon-Carbon bond.
With your reagents you will get not selective N-alkylation, so your product will be mix of N-methyl-PEA + N,N-dimethyl-PEA, even if the PEA will be in excess.
2560px-Phenylethyl_Amine_General_Formula_V1.svg.png
 
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Osmosis Vanderwaal

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This is the unicorn. Once, I read a 1913 patent, that described a method, but reagent they used isn't available commercially. Imwish I would have saved that result, imwas about 3 hours deep in Google patents and had went through about 10 different ways to say it. It was earlier in my pursuit of chemistry, probably last year 🤪
 

Osmosis Vanderwaal

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The mechanism that one uses on ketone and aldehydes don't work here? Could you add a bond on beta and do the ketone flip?
 

FENTAMAS

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@Frit Buchner, no. You can check this list of possible organic reactions - https://en.wikipedia.org/wiki/List_of_organic_reactions and decide what could be the most elegant way to transform your useless PEA to something more interesting (except fentanyls of course).
I assume ring mono- or di-nitration, followed by reduction, side chain amine protection, Sandmeyer reaction, additional haloganation and/or swap of halide(s) for methoxy group(s), side chain amine deprotection, and finally N-benzylation could do the trick.
 

Kj12

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at first thank you for the answer but what if you leave out or replace the potassium carbonate because then there will be no base, and the N-methylation might not occur, or try to protect the nitrogen group?
 
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