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



李国成a,b, 杨爱梅a, 毛卓亚b, 周祝b, 魏邦国b   

  1. 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
  • 基金资助:


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

Li Guochenga,b, Yang Aimeia, Mao Zhuoyab, Zhou Zhub, Wei Bangguob   

  1. 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).

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.

Key words: antipsychotics, asymmetric synthesis, selectivity, nemonapride