生物还原反应在手性药物不对称合成中的应用

药物分子的立体化学决定了其生物活性,手性已成为药物研究的一个关键因素。利用“环境友好”的微生物或酶催化方法进行手性药物的不对称合成已成为一个极具吸引力的方向。而微生物催化还原前手性羰基则可以不对称的得到手性的羟基,用于光学活性手性药物的合成。综述了近年来利用生物还原方法进行制备量和商业规模的不对称合成手性药物的进展。

Application of bioreduction to the asymmetric synthesis of chiral drugs

As stereochemistry in drug molecule governs its biological activity, chirality is emerging as a key issue in pharmaceutical research. It has become attractive to asymmetrically synthesize of chiral drugs through "environmentally friendly" biotransformations. bioreduction of prochiral ketones could enantioselectively lead to chiral alcohols as the intermediates in fruther syntheis of chiral drugs. This review covers the application of bioreduction to the saymmetric synthesis of pharmacologically active compounds on a alboratory and a commercial scale.