CRCU

Chemical Research in Chinese Universities ›› 2012, Vol. 28 ›› Issue (1): 70-72.

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Chemoenzymatic Synthesis of Ramosetron Hydrochloride

LIU Qing-wen1, XU Hao1, TIAN Hua1, ZHENG Liang-yu2*, ZHANG Suo-qin1*   

  1. 1. College of Chemistry, Jilin University, Changchun 130012, P. R. China;
    2. Key Laboratory for Molecular Enzymology and Engineering, Ministry of Education, Jilin University, Changchun 130012, P. R. China
  • Received:2011-03-10 Revised:2011-03-25 Online:2012-01-25 Published:2011-12-27
  • Supported by:

    Supported by the National Natural Science Foundation of China(No.20802025) and the Jilin Provincial Science & Technology Sustentation Program, China(Nos.20090585, 20100538).

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Abstract: A new method for the synthesis of ramosetron hydrochloride, the most wildly used 5-HT3 receptor antagonist, was reported. The intermediate 8 was obtained in a high e.e. value via lipase catalyzed hydrolytic kinetic resolution. Then enantiomerically pure ramosetron hydrochloride was synthesized in two steps with excellent yield (the total yield is 24.6%). The method provides a new environment friendly and atom economy way to synthesize enantiomerically pure ramosetron.

Key words: Ramosetron hydrochloride, Chemical enzymatic synthesis, Atom economy