Over the years, a wide range of stereoselective synthetic methods have found applications in the large-scale asymmetric synthesis of active pharmaceutical ingredients (APIs). As a result, industrial process chemists have come to appreciate the value of these catalytic methods for the development of cost-effective, scalable, and environmentally sound processes, and have started to integrate these technologies into many API syntheses. In addition to a few well-established asymmetric catalytic protocols such as asymmetric hydrogenation and asymmetric epoxidation, many other types of catalytic transformations, such as asymmetric C-C bond-forming and dynamic kinetic resolution approaches, are slowly beginning to be incorporated into the large-scale synthesis of APIs.