新型降血脂药物依替米贝制备技术研究进展  

Research Progress in Preparation Technique of Cholesterol-lowering Drug Ezetimibe

作　　者：金保军[1] 孙婧[1] 何军邀[2] 黄金[1] 王普[1] 

机构地区：[1]浙江工业大学药学院,浙江杭州310014 [2]浙江医药高等专科学校,浙江宁波315100

出　　处：《浙江化工》2015年第11期15-21,共7页Zhejiang Chemical Industry

基　　金：NK1-受体拮抗剂类药物重要手性中间体的生物合成关键技术研究(浙江省科技厅基金项目;Z014C33274)

摘　　要：依替米贝是一种新型选择性胆固醇吸收抑制剂类降血脂药物。该药物的合成有多种方法,本文主要综述了依替米贝合成技术的研究进展,概述了包括不对称催化合成、手性源法、手性拆分、色谱分离和生物不对称合成等有关制备方法。并对今后依替米贝制备技术发展方向进行了展望。Ezetimibe is a novel selective cholesterol absorption inhibitor. Several synthetic methods are reported for the preparation of Ezetimibe. This paper reviewed the synthetic process of Ezetimibe, and summarized the preparation methods such as asymmetric catalytic synthesis, chiral pool synthesis, chiral resolution, chromatographic separation and asymmetrically biocatalytic synthesis. It provided scientific outlook on the development direction for the preparation of Ezetimibe in the future.

关 键 词：依替米贝 降血脂药 不对称合成 生物不对称合成 

分 类 号：TQ460.6[化学工程—制药化工]