Ligand‐Accelerated Direct C−H Arylation of BINOL: A Rapid One‐Step Synthesis of Racemic 3,3′‐Diaryl BINOLs

Abstract

Abstract An ortho ‐selective rhodium‐catalyzed direct C−H arylation of 1,1′‐bi‐2‐naphthol (BINOL), to deliver the widely used but not easily available 3,3′‐diaryl BINOL, has been developed. This highly efficient one‐step synthetic approach is the shortest route to date and is greatly facilitated by the newly developed ligand system comprising t Bu 2 PCl, Ph 2 ‐cod, and Cy 3 P⋅HBF 4 . In addition, the same procedure can facilitate the challenging syntheses of 3‐bulkyaryl BINOLs in good to excellent yields.