KIO3-Mediated γ-C(sp3)–H Sulfenylation of Enaminones

A metal-free regioselective γ-C(sp3)–H sulfenylation of enaminones with heterocyclic thiols is reported. This transformation is efficient, mild, scalable, and environmentally friendly and tolerates a large variety of enaminones substrates and heterocyclic thiols. The utility of this strategy is demonstrated in a late-stage modification of bioactive natural products and drug derivatives.