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

doi:10.6023/cjoc201604030

Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (9): 2157-2161.DOI: 10.6023/cjoc201604030 Previous Articles Next Articles

ARTICLE

抗精神病药(2S,3S)-奈莫必利的高效合成

李国成^a,b, 杨爱梅^a, 毛卓亚^b, 周祝^b, 魏邦国^b

a 兰州理工大学生命科学与工程学院兰州 730050;
b 复旦大学药学院上海 201203

收稿日期:2016-04-14 修回日期:2016-04-26 发布日期:2016-05-17
通讯作者: 杨爱梅, 魏邦国 E-mail:bgwei1974@fudan.edu.cn
基金资助:
国家自然科学基金（Nos.21072034，21472022，21272041）资助项目.

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

Received:2016-04-14 Revised:2016-04-26 Published:2016-05-17
Supported by:
Project supported by the National Natural Science Foundation of China (Nos.21072034, 21472022, 21272041).

1. Effective Method for Synthesis of Antipsychotics (2S,3S)-Nemonapride.PDF(367KB)

Abstract

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.

Key words: antipsychotics, asymmetric synthesis, selectivity, nemonapride

Cite this article

Li Guocheng, Yang Aimei, Mao Zhuoya, Zhou Zhu, Wei Bangguo. Effective Method for Synthesis of Antipsychotics (2S,3S)-Nemonapride[J]. Chin. J. Org. Chem., 2016, 36(9): 2157-2161.

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抗精神病药(2S,3S)-奈莫必利的高效合成

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

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