Pd/Chiral PhosphoricAcid-Enabled Asymmetric IntramolecularDouble C–H Activation Reaction for the Synthesis of <i>P</i>‑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 <i>P</i>-stereogenic benzophosphole oxides were synthesized in moderate to excellent yield with high levels of enantioselectivity (≤96% ee).