摘要
目的优化(2R,4R)-4-甲基-2-哌啶甲酸乙酯的合成工艺。方法以S-(-)-α-甲基苄胺为原料,与乙醛酸乙酯反应得到[(S)-1-苯乙基亚胺基]乙酸乙酯,与异戊二烯进行环合后,再经不对称氢化和脱保护反应制得(2R,4R)-4-甲基-2-哌啶甲酸乙酯。结果总收率从17.0%提高至47.6%。结论本工艺可有效地降低生产成本。
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.
出处
《中南药学》
CAS
2012年第8期588-590,共3页
Central South Pharmacy
