Abstract: During the past few decades, active pharmaceutical ingredients are becoming increasingly complex and costly to synthesize. Development of sustainable, greener and economically viable manufacturing processes is demanding. Asymmetric catalytic transformations with the aid of chiral phosphine ligands have played a critical part for API development. This lecture will be centered on our recent chiral ligands development, and application for designing an ideal synthesis for an 11β-HSD 1 inhibitor utilizing sequential C-H arylation and a novel enantioselective hydrogenation (Org. Lett. 2018, 20, 1333; J. Am. Chem. Soc. 2016, 138, 15473).