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First synthesis and characterization of SRR/RSS-Ezetimibe
Authors:Yun Ren  RenJun Li  Yong Deng  Mei Guan  Yong Wu  Li Hai
Institution:1. Key Laboratory of Drug Targeting and Drug Delivery Systems, West China School of Pharmacy, Sichuan University, Chengdu 610041, PR China;2. West China Hospital, Sichuan University, Chengdu 610041, Sichuan, PR China
Abstract:The two stereoisomers, SRR-Ezetimibe 2 and RSS-Ezetimibe 3 are related substances of the cholesterol absorption inhibitor drug Ezetimibe 1. Herein, we present an efficient and practical synthesis approach to deliver these two stereoisomers for the first time, and a proof of SRR-Ezetimibe 2 by single-crystal X-ray analysis. Our research will be of immense help for organic chemists to study the impurity profile of Ezetimibe 1.
Keywords:Ezetimibe  SRR-Ezetimibe  RSS-Ezetimibe  Synthesis  X-ray structure
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