摘要
依折麦布是有效的口服降胆固醇药物,属于胆固醇吸收抑制剂类型。依折麦布分子的关键结构为手性β-内酰胺环和侧链上的手性羟基。手性β-内酰胺环的合成策略主要有加成法(Staudinger反应、Kinugasa-Hashimoto反应等)和分子内关环法(酯的胺解)等。手性羟基的合成方法主要有羰基不对称还原法和环氧乙烷还原法等。本文根据这2个关键结构的合成方法对已报道的16条依折麦布的合成路线进行了概述。
Ezetimibe is an effective oral cholesterol-lowering drug,belonging to the type of cholesterol absorption inhibitors.The key frameworks of ezetimibe are chiralβ-lactam ring and chiral hydroxyl group on side chain.The synthetic strategies ofβ-lactam ring include addition(Staudinger reaction,Kinugasa-Hashimoto reaction,etc.),and intramolecular ring closure(aminolysis of esters).The synthetic methods of chiral hydroxyl group mainly include carbonyl asymmetric reduction,and ethylene oxide reduction.In this paper,sixteen synthetic routes of ezetimibe according to the synthetic methods of the two key frameworks were summarized.
作者
高中强
张海峰
秦龙
何凯敏
GAO Zhongqiang;ZHANG Haifeng;QIN Long;HE Kaimin(Xi'an Gelan Xintong Pharmaceutical Co.,Ltd.,Xi'an 710077;Xi'an Xintong Pharmaceutical Research Co.,Ltd.,Xi'an 710077)
出处
《中国医药工业杂志》
CAS
CSCD
北大核心
2020年第8期956-973,共18页
Chinese Journal of Pharmaceuticals
基金
陕西省科技计划项目(2017ZDXM-SF-040)。
关键词
依折麦布
合成
研究进展
ezetimibe
synthesis
research progress
