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Chemical Research in Chinese Universities ›› 2012, Vol. 28 ›› Issue (5): 833-836 .

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Improved Method for Lacosamide Synthesis with Chemoenzymatic Method

WANG Zhi-yuan, XU Li-sheng, LIU Jun-zhong, ZHANG Hong-juan, GAO Ji, LIU Qian, JIAO Qing-cai   

  1. State Key Laboratory of Pharmaceutical Biotechnology, School of Life Science,Nanjing University, Nanjing 210093, P. R. China
  • Received:2012-02-13 Revised:2012-03-23 Online:2012-09-25 Published:2012-09-07
  • Supported by:
    Supported by the National Technology-Innovation Fund(No.02CJ-13-01-16) and the Open Fund of State Key Laboratory of Pharmaceutical Biotechnology of Nanjing University, China.

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Abstract: Lacosamide was prepared by chemical method coupled with enzymatic method. N-Acetyl-D, L-3-methoxy-alanine, derived from D,L-3-methoxy-alanine, was used in the resolution process catalyzed by immobilized Escherichia coli cells with aminoacylase(EC3.5.1.14) activity. N-Acetyl-D-3-methoxy-alanine and L-3- methoxy-alanine were obtained from the resolution system. Lacosamide was synthesized by the amidation of N-acetyl-D-3-methoxy-alanine with benzylamine.

Key words: Lacosamide, Aminoacylase, N-Acetyl-D,L-3-methoxy-alanine, Immobilized cell