Abstract:

Synthesis of chiral drugs and intermediates catalyzed by enzyme has high efficiency，energy saving and environment-friendliness advantages. This paper reviews the solvent effect on the enzymatic reaction in non-aqueous media with lipases，namely，the activity and enantioselectivity of enzyme adjusted by solvent system to improve the efficiency of catalytic reaction. The kinetically controlled synthesis of β-lactam antibiotics with penicillin G acylase was introduced in different solvent systems，including the organic-water miscible solvents，organic-water immiscible solvents，reverse micelles and aqueous two-phase system. The yield of kinetically controlled synthesis of β-lactam antibiotics and synthesis/hydrolysis ratio（S/H）could be enhanced by designing an effective solvent system to better utilize the substrates.

摘要：

生物酶催化合成手性药物和中间体具有高效、节能和环境友好等突出的优势，本文从提高催化反应效率的角度，评述了非水相酶催化反应的溶剂效应——溶剂体系对酶的活性和对映选择性的调控作用；介绍了动力学控制合成β-内酰胺类抗生素的不同溶剂体系，包括有机物-水共溶剂体系、有机物-水不共溶剂体系、反胶束体系和双水相体系。提出利用溶剂效应调控动力学合成体系，会有效提高酶催化合成β-内酰胺类抗生素的产率和合成与水解比S/H值，从而实现底物的有效利用。