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不对称合成与转化——药物合成中手性倍增的工具。

Asymmetric syntheses and transformations--tools for chirality multiplication in drug synthesis.

作者信息

Gawroński Jacek

机构信息

Department of Chemistry, A. Mickiewicz University, 60-780 Poznań, Poland.

出版信息

Acta Pol Pharm. 2006 Sep-Oct;63(5):333-51.

Abstract

A review of currently used methods for the synthesis and resolution of enantiomers of drugs and their precursors is presented. For the synthesis part the methods of diastereoselective as well as enantioselective synthesis are discussed, with particular consideration given to enantioselective catalysis with either metal complexes or biocatalysts. Desymmetrization processes are also included as methods to access enantiomerically pure compounds. Racemate resolution still remains an important method to obtain pure enantiomers and methods involving kinetic resolution in enzymatic or chemical systems, and particularly in connection with racemization (dynamic kinetic resolution) are on the rise in fine chemical industry, when applicable.

摘要

本文综述了目前用于药物及其前体对映体合成与拆分的方法。在合成部分,讨论了非对映选择性合成和对映选择性合成方法,特别考虑了使用金属配合物或生物催化剂的对映选择性催化。去对称化过程也作为获得对映体纯化合物的方法被纳入其中。外消旋体拆分仍然是获得纯对映体的重要方法,涉及酶促或化学体系中动力学拆分的方法,特别是与外消旋化相关的方法(动态动力学拆分)在精细化工行业中应用时正在兴起。

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