Z. Can
2012
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Journal
Central South Pharmacy
Abstract
Objective To optimize the synthesis of ethyl(2R,4R)-4-methylpi-peridine-2-carboxylate.Methods Ethyl(2R,4R)-4-methylpiperidine-2-carboxylate was synthesized from(S)-1-phenylethanamine and ethyl 2-oxoacetate to obtain ethyl [(S)-1-phenylethylimino]acetate,which underwent cyclization with isoprene followed by asymmetric hydrogenation and deprotection.Results The overall yield was improved from 17.0% to 47.6%.Conclusion This method is effective for reducing production costs.