Sulfonium Salt-Mediated Regio- and Stereoselective Aminosulfonylation of Alkynes with Sulfinates and Azoles

In this study, a practical and efficient one-pot sulfonium salt-mediated regio- and stereoselective aminosulfonylation of alkynes with sulfinates and azoles has been established. This method enables the synthesis of structurally diverse N-heterocycle-containing (<i>Z</i>)-vinyl sulfones, featuring a broad substrate scope and excellent functional group tolerance. Notably, gram-scale synthesis, product derivatization, and late-stage functionalization further validate the synthetic utility of this protocol, thereby rendering it highly valuable for applications in organic synthesis and medicinal chemistry.