Heterocycle Synthesis Based on Palladium-Catalyzed C-H Bond Functionalization Methods

This Review reports recent developments in the synthesis of benzo-fused heterocycles through Pd-catalyzed carbon-carbon and carbon-heteroatom bond forming reactions via direct C-H activation. Nitrogen-, oxygen- and sulfur-containing heterocyclic rings can be rapidly assembled starting from precursors with minimal preactivation. Compared to classical coupling reactions (i.e. Suzuki, Stille, Buchwald-Hartwig), these methods provide a more straightforward and economical route to various heterocyclic scaffolds, which is of practical importance considering their role in biology and pharmaceutical industry.