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The increasing trend of chiral drugs in the pharmaceutical industry has promoted greatly on the development of numerous biocatalytic routes in combination with chemical methods. Because the resulting chiral alcohols are particularly valuable intermediates and precursors for the synthesis of chiral drugs, dehydrogenases and reductases have been extensively used in the synthesis of chiral compounds from ketone substrates with high regio- and stereo-selectivities. In this review, biocatalytic processes carried out by dehydrogenases and reductases are described for the synthesis of chiral intermediates for a wide variety of pharmaceuticals, including antidepressants, anti-anxieties, anti-asthmatics, anti-hypertensives, cholesterol-lowering agents, NK1 antagonists, ACE inhibitors and β- Lactamase inhibitors.