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