How to: 2-Carbomethoxytropinone to Methylecgonine?

[e***@gmail.com]

It's all about the cocaine?

[g***@gmail.com]

Hello,
I have synthesized 1034 grams of 2-Carbomethoxytropinone (It has
costed me a $1950, I can give you a list of suppliers I've used), and
I am stuck with converting it to methylecgonine.
Could anyone advise which method to use, references to some papers
would be helpfull.
What is the ratio? like 100grams would convert into X grams of
methylecgonine?

Homebrew cocaine starts by purchasing or making tropinone, converting
the tropinone into 2-carbomethoxytropinone (also known as
methyl-tropan-3-one-2-carboxylate), reducing this to ecgonine, and
changing that to cocaine. Since there is no optical isomer selection
anywhere in the path, the resulting "cocaine" is a mixture of 8
isomers (the two bridgehead chiral centers are linked) and quite
worthless. Some of the isomers are toxic.
--
Uncle Al
http://www.mazepath.com/uncleal/
(Toxic URL! Unsafe for children and most mammals)
"Quis custodiet ipsos custodes?" The Net!

[dr jack Mathew]

Hello,
I have synthesized 1034 grams of 2-Carbomethoxytropinone (It has
costed me a $1950, I can give you a list of suppliers I've used), and
I am stuck with converting it to methylecgonine.
Could anyone advise which method to use, references to some papers
would be helpfull.
What is the ratio? like 100grams would convert into X grams of
methylecgonine?
Thanks,
Dustin

Great work, Besides the classic findlay paper there is a paper in JOC in 1974 from university of Davis professor Bottini who makes Tropinone in 2 steps from the readily available cycoheptanone and bromine followed by double Michael addition of methyl amine to give tropinone in excellent yield. This can be acylated to 2-carbomethoxy tropinone by sodium or potassium ethoxide and dimethyl carbonate as mentioned in 1953 Findlays article. Optical resoltion followed by sodium amalgam reduction results in the desired enantiomer of cocaine which on benzoylation gives pure cocaine