Palladium-catalyzed alkynylative [5 + 1] carboannulation of 1,3-diarylprop-2-yn-1-yl acetates with terminal alkynes enabled by C–H functionalization

Abstract

A new method for the synthesis of 3-ethynyl-1-methylene-1,2-dihydronaphthalenes via copper-promoted palladium-catalyzed intermolecular alkynylative [5 + 1] carboannulation of 1-arylphenyl-prop-2-yn-1-yl acetates involving C–H functionalization is described. Two terminal alkyne molecules serve as an alkynylation reagent and a one-carbon unit to enable alkynylative [5 + 1] carboannulation with excellent selectivity control, broad substrate scope and good tolerance of functional groups.