Abstract

Herein, we report a highly efficient organocatalytic asymmetric arylation of p-quinone phosphonates and 2-naphthols. A series of chiral biaryl monophosphonates were obtained under mild conditions in excellent yields and enantionselectivities (up to 99% yield and 95% ee). This reaction is highly functional group tolerant and could be operated at gram scale with a low catalyst loading (0.5 mol %). Remarkably, our approach provides a green and readily access to novel chiral biaryl monophosphorus ligands. Compound 4ca was successfully converted to novel chiral biaryl monophosphorus ligands 7a, 7b and 8 with high enantionselectivities in three steps.

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