Discovery and Utilization of Biocatalysts for Chiral Synthesis: An Overview of Chinese Scientists Research and Development

Abstract

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.

Complete Genome Sequence of Sphingorhabdus sp. YGSMI21, Exhibiting High Enantioselective Epoxide Hydrolase Activity

“…In chiral compounds, it is common for biological activities to occur in one enantiomer, while other enantiomers have no activity or adverse side effects ( 4 ). Since pharmaceuticals with a chiral carbon should be developed as a single enantiomer ( 5 , 6 ), there is a need for continuous study to find microbial sources of enantioselective EHase that preferably hydrolyze only one enantiomer in racemic substrates ( 1 ). EHase with a desired enantioselectivity has been screened from polycyclic aromatic hydrocarbon-degrading bacteria, resulting in the isolation of the novel strain Sphingorhabdus sp.…”