Chirality is a key factor in the safety and efficacy of many drug products and thus producing single enantiomers of drug intermediates and drugs has become increasingly important in the pharmaceutical industry. There has been an increasing awareness of the enormous potential of microorganisms and enzymes derived from them for the transformation of synthetic chemicals with high chemo-, regio-, and enatioselectivities. In this article, biocatalytic processes are described for the synthesis of key chiral intermediates for development of pharmaceuticals and fine chemicals.