1,4-二氢吡啶衍生物的手性拆分及不对称合成进展  

Progress in chiral resolution and asymmetrical synthesis of 1,4-dihydropyridine derivatives

作　　者：卢定强[1,2] 常亚军[1] 凌岫泉[1] 陈佳[1] 赵鹏[1] 王加力[1] 

机构地区：[1]南京工业大学药学院,江苏南京210009 [2]江苏省药物研究所,江苏南京210009

出　　处：《化工进展》2010年第12期2351-2361,2378,共12页Chemical Industry and Engineering Progress

基　　金：国家自然科学基金(20676060);国家重点基础研究发展计划(2009CB724700)资助项目

摘　　要：1,4-二氢吡啶衍生物(1,4-DHPs)具有广泛的生物活性,是重要的钙离子拮抗剂,详细介绍了拆分法以及不对称合成法制备光活性1,4-二氢吡啶衍生物的研究进展。拆分有化学拆分和酶拆分两种,化学拆分法主要包括经典成盐法和形成非对映体酯法,用于拆分1,4-DHPs的酶有脂肪酶和蛋白酶两种。分析了几种方法的优缺点,提出了今后的发展方向。1,4-Dihydropyridine derivatives（1,4-DHPs）possess a wide range of biological activities,which is an important calcium channel blocker.This review summarizes recent studies in the chiral resolution and asymmetrical synthesis of 1,4-dihydropyridine derivatives.The chiral resolution can be classified as chemical resolution and enzymatic kinetic resolution,the former includes classical method of resolution and separation via diastereomeric ester,and the latter is catalyzed by lipase and protease.Advantages and disadvantages of each resolution method are analyzed,and prospects for future development are discussed.

关 键 词：1 4-二氢吡啶 拆分 不对称合成 

分 类 号：O626.32[理学—有机化学]