Toward an Ideal Synthesis of (Bio)molecules through Direct Arene Assembling Reactions

C–H (hetero)arylation of aromatic compounds using transition-metal catalysts has garnered much attention from the synthetic chemistry community as a next-generation coupling method for constructing (hetero)biaryl motifs. This account describes our recent achievements in transition-metal-catalyzed aromatic C–H arylation and its applications to the synthesis of bioactive molecules.