Radical-Mediated Sulfonylarylation of Unactivated Alkynes via Intramolecular 1,4-(hetero)aryl Migration

Abstract

Radical-mediated difunctionalization of alkynes is an extensively explored strategy for diverse alkyne transformation and utilization. However, the direct difunctionalization of unactivated alkynes remains a significant challenge. In this study, a novel visible light-induced, redox-neutral sulfonylarylation of unactivated alkynes is reported, facilitated by a radical-mediated intramolecular 1,4-(hetero)aryl migration. Notably, this transformation enables the synthesis of a diverse array of multisubstituted vinyl sulfones, with tunable (E)- and (Z)-selectivity controlled by the wavelength of visible light. This method features mild reaction conditions, excellent regio- and stereoselectivity, and broad functional group compatibility.