State Key Laboratory of Bioreactor Engineering, East China University of Science and Technology, 130 Meilong Road, Shanghai, 200237, China.
Adv Biochem Eng Biotechnol. 2009;113:1-31. doi: 10.1007/10_2008_30.
The importance of chiral issues in active pharmaceutical ingredients has been widely recognized not only by pharmacologists, but also by chemists, chemical engineers and administrators. In fact, the worldwide sales of single-enantiomer drugs have exceeded US $150 billion. Among them the contribution rate of biocatalysis technology is ever increasing (up to 15-20%). This chapter will focus on the biocatalytic synthesis of chiral compounds useful for pharmaceutical industry. Diverse enzymes, such as oxidoreductases, epoxide hydrolases, nitrilases/nitrile hydratases and hydroxy nitrile lyases which were isolated from various sources including microorganisms and plants, and the methodology for utilizing these enzymes in enantioselective or asymmetric synthesis will be discussed briefly.
手性问题在原料药中的重要性不仅被药理学家广泛认可，也被化学家、化学工程师和管理人员广泛认可。事实上，单一对映体药物的全球销售额已经超过 1500 亿美元。其中，生物催化技术的贡献率不断增加（高达 15-20%）。本章将重点介绍用于制药工业的手性化合物的生物催化合成。简要讨论了从微生物和植物等各种来源分离出的氧化还原酶、环氧化物水解酶、腈酶/腈水合酶和羟基腈裂解酶等多种酶，以及利用这些酶进行对映选择性或不对称合成的方法。
