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.2c02824 | DOI Listing |
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