B. Hao, Jinqiang Liu, Weihan Zhang
Apr 1, 2011
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Journal
Synthesis
Abstract
CIS-(3 R,4 R)- N-( TERT-Butoxycarbonyl)-4-methyl-3-(meth-ylamino)piperidine,a key intermediate for the synthesis of CP-690550 (a potent proteinkinase inhibitor), is prepared via an asymmetric approach startingfrom ethyl 1-benzyl-3-oxopiperidine-4-carboxylate hydrochloridein an overall yield of 49%. The mild conditions and highyields obtained during the synthesis suggest a potential industrialapplication for this route.