Construction of Biologically Important Biaryl Scaffolds through Direct C–H Bond Activation: Advances and Prospects

Abstract: Biaryl scaffolds are prevalent in natural products and drug molecules, and biaryl-containing compounds have been shown to exhibit diverse and interesting biological activities. To date, numerous synthetic methods, particularly direct C–H bond activation, have been developed for the construction of such scaffolds, due to their interesting structural features and biological profiles. We highlight herein recent advances in the construction of biologically important biaryl fragments through direct C–H bond activation and also demonstrate the application of direct C–H arylation in the total synthesis of biaryl-containing natural products and drug molecules.