Pd/Chiral Phosphoric Acid-Enabled Asymmetric Intramolecular Double C–H Activation Reaction for the Synthesis of P-Stereogenic Benzophosphole Oxides

A Pd-catalyzed intramolecular asymmetric double C-H activation reaction was reported, and a BINOL skeleton-based chiral phosphoric acid (CPA) was identified as a suitable ligand for this transformation. A broad range of P-stereogenic benzophosphole oxides were synthesized in moderate to excellent yield with high levels of enantioselectivity (≤96% ee).