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Chin. J. Org. Chem. ›› 2007, Vol. 27 ›› Issue (07): 857-861. Previous Articles     Next Articles

Original Articles

有机相酶催化拆分制备(S)-2-氯-1-(2-噻吩)-乙醇

徐刚，程咏梅，吴坚平，杨立荣*   

  1. (浙江大学材料与化学工程学院 杭州 310027)
  • 收稿日期:2006-12-21 修回日期:1900-01-01 发布日期:2007-06-30
  • 通讯作者: 杨立荣*

Preparation of (S)-2-(2-Chloro-1-hydroxyethyl)thiophene by Lipase-Catalyzed Resolution in Organic Phase

XU Gang,CHEN Yong-Mei,WU Jian-Ping,YANG Li-Rong*   

  1. (College of Material Science and Chemical Engineering, Zhejiang University, Hangzhou 310027)
  • Received:2006-12-21 Revised:1900-01-01 Published:2007-06-30
  • Contact: YANG Li-Rong*

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The kinetic resolution of 2-(2-chloro-1-hydroxyethyl)thiophene in organic phase, catalyzed by lipase, was firstly investigated. Through screening lipases, lipase Novozym 435 and lipase Alcaligenes sp were found to show higher activity and better enantioselectivity for the resolution of 2-(2-chloro- 1-hydroxyethyl)thiophene. The optimal reaction conditions were finally achieved by further investigating the effects of solvents, temperature, rotation speed and enzyme concentrations. 98.5% ee value of (S)-2- (2-chloro-1-hydroxyethyl)thiophene with 48.6% yield could be achieved after 72.5 h when the temperature was 35 ℃ and the concentration of lipase was 10 mg/mL.

Key words: duloxetine, resolution, lipase-catalyzed, (S)-2-(2-chloro-1-hydroxyethyl)thiophene