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高等学校化学研究 2012, Vol. 28 Issue (1) :70-72    DOI:
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Chemoenzymatic Synthesis of Ramosetron Hydrochloride
LIU Qing-wen1, XU Hao1, TIAN Hua1, ZHENG Liang-yu2*, ZHANG Suo-qin1*
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

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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.
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LIU Qiang-Wen
XU Hao
TIAN Hua
ZHENG Liang-Yu
ZHANG Suo-Qin
KeywordsRamosetron hydrochloride   Chemical enzymatic synthesis   Atom economy     
Received 2011-03-10; published 2011-12-27
Fund:

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

Cite this article:   
LIU Qing-wen, XU Hao, TIAN Hua, ZHENG Liang-yu, ZHANG Suo-qin.Chemoenzymatic Synthesis of Ramosetron Hydrochloride[J]  高等学校化学研究, 2012,V28(1): 70-72
URL:  
http://www.cjcu.jlu.edu.cn/hxyj//EN/     or     http://www.cjcu.jlu.edu.cn/hxyj//EN/Y2012/V28/I1/70
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