Journal
TETRAHEDRON LETTERS
Volume 54, Issue 48, Pages 6443-6446Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.tetlet.2013.09.049
Keywords
Ezetimibe; SRR-Ezetimibe; RSS-Ezetimibe; Synthesis; X-ray structure
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Funding
- Sichuan provincial science and technology support program [2011SZ0014]
- Sichuan Bali Pharmaceutical Co., Ltd.
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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. (C) 2013 Elsevier Ltd. All rights reserved.
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