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.