doi:10.16597/j.cnki.issn.1002-154x.2023.01.005
恩格列净制备过程中一种手性脱碘杂质的合成与表征
蒙利民1,2 范钢2,3 吴利鑫2,3 沈莎莎2,3 罗艳娟1,3 商甜波1,3 沈华良1,3∗
(1. 绍兴文理学院,浙江 绍兴 312000;2. 浙江医药股份有限公司,浙江 绍兴 312300; 3. 脂溶性维生素浙江省工程研究中心,浙江 绍兴 312000)
Synthesis and Characterization of a Chiral Deiodinated Impurity Derived from the Preparation of Empagliflozin
Meng Limin 1,2; Fan Gang 2,3; Wu Lixin 2,3; Shen Shasha 2,3; Luo Yanjuan 1,3; Shang Tianbo 1,3; Shen Hualiang 1,3∗;
(1. Shaoxing University, Zhejiang Shaoxing 312000; 2. Zhejiang Medicine Co. ,Ltd. , Zhejiang Shaoxing 312300; 3. Zhejiang Engineering Research Center of Fat-soluble Vitamin, Zhejiang Shaoxing 312000)
摘要:
目的:报道了恩格列净制备过程中一种手性脱碘杂质的合成方法,并对其进行了表征。 为控制恩格列净的产品质量,本研究基于其生产工艺,分离提纯了一种手性脱碘杂质,通过1 H-NMR、 13 C-NMR 等表征确定了结构。 同时,设计了一条新路线高效合成了该杂质,以期为恩格列净原料药的质量和安全性研究提供技术支持。
关键词：恩格列净；质量；手性脱碘杂质；合成；
Abstract：
A chiral deiodinated impurity of an intermediate of empagliflozin was synthesized and characterized in this study. Firstly, the deiodinated impurities of the intermediate was separated and characterized by 1H - NMR, 13C - NMR, et al. Then, an efficient route to access the impurity was developed, which provides a technical support for the quality and safety study of empaliflozin.
Keywords：Empagliflozin; quality; chiral deiodinated impurity; synthesis;