Strategic Advances in Sequential C-Arylations of Heteroarenes

Sequence-specific C-arylation strategies have important applications in medicinal and material research. These strategies allow C-C bond formations in a regioselective manner to synthesize large molecular libraries for studying structure-activity profiles. The past decade has seen the development of single C-C bond forming reactions using various transition-metal catalysts, cryogenic metalation strategies, and metal-free methods. Sequential arylations of heterocycles allow for the formation of multiaryl derivatives and are a preferred choice over de novo synthetic routes. This perspective sheds light on recent strategic advances to develop various sequential synthetic routes for the multiarylation of heteroarenes. This perspective addresses many challenges in optimizing sequential routes with respect to catalysts, reaction parameters, and various strategies adopted to obtain diversely arylated products.