Application of Deracemization in Asymmetric Synthesis by Biocatalyst

Liu Zhenzhen1, Ji Aiguo1,2*, Cui Hongjie3
(1College of Pharmacy, Shandong University, Jinan 250012 )
(2Department of Marine Bioengineering , Weihai Campus , Shandong University , Weihai 264209)
(3Bingzhou Teachers College, Bingzhou 256603)

Abstract The deracemization reaction with microbes or enzymes inverts the chirality of one enantiomer of a racemate to the other antipode, resulting in an optically active compound starting from a racemic mixture. Thus this process may obtain 100% yield and enantiomeric excess. However, the most maximum theoretical yield of classical kinetic resolution is limited to 50% and the tedious procedures for the separation of the starting material and the product are inevitable. Accordingly, deracemization as a simple and efficient method has gained more and more attention. In this paper, the application of deracemization in asymmetric synthesis is reviewed.
Key words Deracemization, Chirality, Biocatalysis

　

生物催化去消旋化在不对称合成中的应用

刘珍珍1 吉爱国1,2* 崔宏杰3
(1山东大学药学院 济南 250012 2山东大学威海分校海洋生物工程系 威海 264209 3滨州师专 滨州 256603)

摘要 生物催化去消旋化是利用微生物或酶对底物进行高度立体选择性序列生物转化，得到所需的单一光学异构体的方法，并可达到100%的产率和对映体过量率。而传统的拆分法仅能获得最高50%的产率，还需要繁琐的步骤来分离反应原料和产物。因此，去消旋化作为一个简便而有效的方法越来越得到人们的重视。本文中，笔者就去消旋化在不对称合成中的应用进行了综述。
关键词 去消旋化 手性 生物催化

刘珍珍 女，24岁，硕士生，现从事药物生物合成与生物转化的研究。 *联系人
国家自然科学基金(30270047)和教育回国人员科研启动基金(05200105)资助项目
2003-09-10收稿，2004-02-07接受

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