Hydroxyl-Directed Ruthenium-Catalyzed peri-Selective C-H Acylmethylation and Annulation of Naphthols with Sulfoxonium Ylides.

Herein, we report a highly efficient ruthenium-catalyzed peri-selective C(sp2)-H acylmethylation of 1-naphthols with α-carbonyl sulfoxonium ylides by utilizing hydroxyl as a weakly coordinating directing group. This new method imparts good reactivity, excellent chemo- and regioselectivity, and broad functional group tolerance and involves mild reaction conditions. The C-H acylmethylated products can be readily cyclized into fluorescent annulated pyrans by a one-pot process.