基于邻位叔丁基二甲基硅氧基(OTBS)手性基团诱导的亚胺(R,SRS)-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.