Abstract

Hydrolases are versatile enzymes for synthetic purposes as they are able to catalyze multiple transformations in both aqueous medium and organic solvents. Their easiness of use and lack of cofactor dependency have attracted the attention of many organic chemists, which have successfully applied this family of enzymes in hydrolytic and reverse synthetic reactions. In this review, the authors have focused on the recent application of hydrolases for the synthesis of active pharmaceutical ingredients and different families of compounds with exceptional biological profiles. Thus, their action has been classified in non-selective and selective transformations including regio- and stereoselective processes. Asymmetric transformations are presented as key issues for the production of drug enantiomers, so examples of hydrolase-catalyzed kinetic resolutions, dynamic kinetic resolutions and desymmetrizations will be extensively discussed, presenting hydrolases as very versatile enzymes for the development of scalable synthetic transformations towards pharmaceuticals.

Keywords: Asymmetric synthesis, biotransformations, desymmetrization, hydrolases, kinetic resolutions, pharmaceuticals.

Graphical Abstract