The catalytic asymmetric hydrogenation, which features with perfect atom-efficiency, clean, and high efficiency, represents one of the most practical reactions in modern organic synthesis. Although tremendous efforts have been devoted into this field, few of chiral catalysts showed both high reactivity and high enantioselectivity to date. In this project we developed more than 30 chiral catalysts, which were successfully applied in the enantioselective hydrogenation reactions of prochiral ketones, α-substituted carbonyl compounds, unsaturated acids, and unprotected enamines. These asymmetric hydrogenation reactions showed high activity and enantioselectivity, and some of them have been successfully applied in the scaled-up synthesis of chiral drugs or the key intermediates.