Li Yuhua
2010
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Journal
Chinese Journal of Pharmaceuticals
Abstract
The central analgesics tapentadol hydrochloride was synthesized from 1-(3-methoxyphenyl)-1-propanone by Mannich reaction with dimethylamine hydrochloride to obtain racemic 3-dimethylamino-1-(3-methoxyphenyl)-2-methylpropan-1-one(13),which was subjected to crystallization-induced diastereomer transformation,Grignard reaction,acylation and catalytic hydrogenolysis to give (2R,3R)-2-methyl-3-(3-methoxyphenyl)-N,N-dimethylpentanamine,followed by deprotection and salt formation with an overall yield of about 52%.