KIO-Mediated γ-C(sp)-H Sulfenylation of Enaminones.

Org Lett

State Key Laboratory of Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Sciences, Kunming 650201, P. R. China.

Published: October 2022

A metal-free regioselective γ-C(sp)-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.

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http://dx.doi.org/10.1021/acs.orglett.2c02824DOI Listing

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