Lipases and esterases are capable of functioning in the presence of water-miscible as well as immiscible solvents. Water is known to be a poor solvent in preparative organic chemistry. The umbrella of biocatalysis is vast enough to cover myriad of industrial applications including detergent formulations, feed and food enzymes, production of biodiesel, and most importantly the production of fine chemicals like agro-chemicals and pharmaceuticals. For improving the efficacy of lipase-mediated biocatalysis, a number of modifications in the enzyme are carried out including enzyme immobilization. Microbial lipases are the most versatile enzymes that can bring about a huge range of bioconversions such as hydrolysis, esterification, transesterification, interesterification, alcoholysis, aminolysis, and acidolysis. Lipase and esterase-aided biotransformations are important for the synthesis of active pharmaceutical ingredients as well as their intermediates. The biocatalytic synthesis of captopril was one of the path breaking achievements of the initial age of biocatalysis.