We have developed the first I2/base-catalyzed
regio-
and stereoselective intermolecular β-amidosulfonylation of terminal
alkynes using sodium sulfinates and quinoxalinone derivatives. The
present methodology is compatible with a broad spectrum of various
heterocyclic amides, terminal alkynes, and sodium sulfinates. It provides
rapid access to valuable (Z)-β-amidovinyl sulfones
at mild conditions. Moreover, the synthetic application of this methodology
was demonstrated by the late-stage functionalization of numerous bioactive
molecules.