Enantioselective Synthesis of Biaryl Atropisomers via Pd/Norbornene-Catalyzed Three-Component Cross-Couplings

Abstract

Three-component cross-coupling cocatalyzed by palladium and norbornene is reported for the synthesis of biaryl atropisomers. This domino reaction gave optimal yield and enantioselectivity with a P,C-type ligand bearing axial chirality and P chiral center. The process showed advantages over traditional cross-coupling because of its step economy and its compatibility with readily available ortho-substituted aryl halides, which could, therefore, be used instead of continuously trisubstituted aryl halides.