1,4-二氢吡啶衍生物的手性拆分及不对称合成进展

化工进展

1,4-二氢吡啶衍生物的手性拆分及不对称合成进展

卢定强1,2，常亚军1，凌岫泉1，陈佳1，赵鹏1，王加力1

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

出版日期:2010-12-05 发布日期:2010-12-05

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

LU Dingqiang 1，2，CHANG Yajun1，LING Xiuquan1，CHEN Jia1，ZHAO Peng1，WANG Jiali1

1 School of Pharmacy，Nanjing University of Technology，Nanjing 210009，Jiangsu，China；2 Jiangsu Provincial Institute of Material Medica，Nanjing 210009，Jiangsu，China

Online:2010-12-05 Published:2010-12-05

摘要/Abstract

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。

Abstract:

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.

卢定强1,2，常亚军1，凌岫泉1，陈佳1，赵鹏1，王加力1. 1,4-二氢吡啶衍生物的手性拆分及不对称合成进展 [J]. 化工进展.

LU Dingqiang 1，2，CHANG Yajun1，LING Xiuquan1，CHEN Jia1，ZHAO Peng1，WANG Jiali1. Progress in chiral resolution and asymmetrical synthesis of 1,4-dihydropyridine derivatives[J]. Chemical Industry and Engineering Progree.