Microwave-Assisted Ru(II)-Catalyzed Regioselective Methyl Acylation of 2‑Arylbenzoazoles: Synthesis of Benzofuran Conjugates via C–H Activation/Annulation

An efficient Ru­(II)-catalyzed C–H functionalization protocol for 2-arylbenzoazoles as the directing group and sulfoxonium ylide has been developed. Gratifyingly, concomitant annulation was observed when 3-(benzo­[d]­azol-2-yl) phenol was used, enabling the construction of benzofuran conjugates. Notably, the utilization of water as the solvent and an energy efficient approach makes the reaction greener, contributing to overall sustainability. This protocol exhibits excellent scalability up to the gram scale with a diverse array of substitutions. Furthermore, the mechanism was examined by ESI-MS, and photophysical studies were also performed.