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

Shaobai Yan, Zhen Li, Hu XianQi, Shuwei Zhang, Wei‐Liang Duan

2025Organic Letters7 citationsDOI

Abstract

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).

Topics & Concepts

StereocenterChemistryPhosphoric acidIntramolecular forceStereochemistryCombinatorial chemistryMedicinal chemistryCatalysisEnantioselective synthesisOrganic chemistryCatalytic C–H Functionalization MethodsAsymmetric Hydrogenation and CatalysisSulfur-Based Synthesis Techniques
Pd/Chiral Phosphoric Acid-Enabled Asymmetric Intramolecular Double C–H Activation Reaction for the Synthesis of <i>P</i>-Stereogenic Benzophosphole Oxides | Litcius