Citation: Yun Ren, Yan-Jun Duan, Ren-Jun Li, Yong Deng, Li Hai, Yong Wu. First synthesis and characterization of key stereoisomers related to Ezetimibe[J]. Chinese Chemical Letters, ;2014, 25(8): 1157-1160. doi: 10.1016/j.cclet.2014.03.035 shu

First synthesis and characterization of key stereoisomers related to Ezetimibe

1.
Key Laboratory of Drug Targeting and Drug Delivery System of the Education Ministry, Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041, China

Corresponding author: Li Hai, Yong Wu,
Received Date: 9 January 2014
Available Online: 12 March 2014
Fund Project: Sichuan Bali Pharmaceutical Co., Ltd. for financial support. (No. 2011SZ0014)

During the laboratory optimization and the late phase manufacturing studies of the cholesterol absorption inhibitor Ezetimibe 1, the formation of several stereoisomers was observed. To study the complete stereoisomer profile of Ezetimibe 1,we have synthesized and completely characterized several key stereoisomers of Ezetimibe 1 for the first time. This study will provide an access to the reference standard of these stereoisomers andmay have some implications in the development of new medicines.
- Ezetimibe,
- Related substances,
- Stereoisomers profile,
- Synthesis,
- Characterization
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沈阳化工大学材料科学与工程学院沈阳 110142