Citation: Li Guocheng, Yang Aimei, Mao Zhuoya, Zhou Zhu, Wei Bangguo. Effective Method for Synthesis of Antipsychotics (2S, 3S)-Nemonapride[J]. Chinese Journal of Organic Chemistry, ;2016, 36(9): 2157-2161. doi: 10.6023/cjoc201604030 shu

Effective Method for Synthesis of Antipsychotics (2S, 3S)-Nemonapride

Li Guocheng ^a,b ,
Yang Aimei ^a ,
Mao Zhuoya ^b ,
Zhou Zhu ^b ,
Wei Bangguo ^b,*,,

a.
College of Life Science and Engineering, Lanzhou University of Technology, Lanzhou 730050
b.
School of Pharmacy, Fudan University, Shanghai 201203

Corresponding author: Wei Bangguo, bgwei1974@fudan.edu.cn
Received Date: 14 April 2016
Revised Date: 26 April 2016

Fund Project: the National Natural Science Foundation of China 21472022the National Natural Science Foundation of China 21272041the National Natural Science Foundation of China 21072034

Figures(3)

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, S_RS)-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.
- antipsychotics,
- asymmetric synthesis,
- selectivity,
- nemonapride
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