Organophosphorus compounds are very useful ligands to coordinate with various transition metals to modulate the catalytic activity and stereoselectivity of reactions. Many recent breakthroughs have been made in synthesizing chiral organophosphorus compounds.[1] Herein, we report the progress in synthesizing organophosphorus compounds based on the C-H bond activation pathway[2]. We investigated phosphorus oxides' asymmetric C-H bond activation reactions by combining chiral phosphine ligands, chiral phosphoric acids, or chiral amides with transition metal catalysts (Scheme 1).