Feng Fengyi , Zhang Pin , He Youjian 1, Li Yuhong1 , Zhou Meizhen2 , Chen Gang2 and Li Lin2 The Cancer Hospital of the CAMS & PUMC, Beijing 1000211 The Cancer Hospital of Sun Yat Sen University of Medical Science...Feng Fengyi , Zhang Pin , He Youjian 1, Li Yuhong1 , Zhou Meizhen2 , Chen Gang2 and Li Lin2 The Cancer Hospital of the CAMS & PUMC, Beijing 1000211 The Cancer Hospital of Sun Yat Sen University of Medical Sciences, Guangzhou 5100602Beijing Hospital of the Ministry of Health, Beijing 100730展开更多
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 re...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.展开更多
文摘Feng Fengyi , Zhang Pin , He Youjian 1, Li Yuhong1 , Zhou Meizhen2 , Chen Gang2 and Li Lin2 The Cancer Hospital of the CAMS & PUMC, Beijing 1000211 The Cancer Hospital of Sun Yat Sen University of Medical Sciences, Guangzhou 5100602Beijing Hospital of the Ministry of Health, Beijing 100730
基金Supported by the National Natural Science Foundation of China(No.20802025)the Jilin Provincial Science & Technol-ogy Sustentation Program, China(Nos.20090585, 20100538)
文摘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.
