摘要
基于邻位叔丁基二甲基硅氧基(OTBS)手性基团诱导的亚胺(R,S_(RS))-8与甲基溴化镁高选择性加成环合串联反应制备4-OTBS-5-甲基吡咯酰胺1的新方法,经叠氮化与缩合等7步反应,以17%的总收率建立了抗精神病药(2S,3S)-奈莫必利选择性合成方法.
An efficient method for the preparation of （4S,5R）-4-（tert-butyldimethylsilyloxy）-5-methylpyrrolidin-2-one （1） by an addition-cyclization-deprotection process of the imine （R,SRS）-8 with Grignard reagent is described. （2S,3S）-Nemonapride, a commercial antipsychotics, was asymmetrically synthesized by a concise and effective route involving above one-pot intramo-lecular tandem protocol in 17% overall yield from 8.
出处
《有机化学》
SCIE
CAS
CSCD
北大核心
2016年第9期2157-2161,共5页
Chinese Journal of Organic Chemistry
基金
国家自然科学基金(Nos.21072034
21472022
21272041)资助项目~~
