摘要
第三代羟甲戊二酰辅酶A(HMG-CoA)还原酶抑制剂——阿托伐他汀是年销售额超过百亿的重磅降血脂药物,因其疗效显著而广受医生患者好评。阿托伐他汀主要通过疏水性母核及手性侧链进行合成,而手性侧链的制备是合成关键。目前,生物催化技术在手性药物合成中的应用备受关注,而阿托伐他汀手性侧链中间体(S)-4-氯-3-羟基丁酸乙酯的酶法合成也成为研究热点。本文主要介绍近年酶法合成在(S)-4-氯-3-羟基丁酸乙酯中的研究进展。
The third generation cholesterol-lowering 3-hydroxy-3-methyl-glutaryl CoA （HMGCoA） reductase inhibitor atovastatin is a kind of critically acclaimed blockbuster drugs with annual sales exceeding billions and significant effect. Atorvastatin is synthesized by the hydrophobic parent nucleus and the chiral side chain, while its key is the preparation of side chain. Currently, the bioeatalysis technology in the synthesis of chiral drugs has been drawn extensive attentions. Moreover, the enzymatic synthesis in the atorvastatin chiral side chain intermediate ethyl （S）-4-chtoro- 3-hydroxybutanoate has been the research hotspot. This paper reviewed the research progress of enzymatic catalysis in the synthesis of ethyl （S）-4-chloro-3- hvdroxvbutanoate.
出处
《发酵科技通讯》
CAS
2014年第3期19-23,共5页
Bulletin of Fermentation Science and Technology
基金
国家重点基础研究发展计划(973计划)(项目编号:2011CB710806)
