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A metal-free protocol for the direct construction of C(sp2)–N and C–O bonds via a PhI(OAc)2-mediated dehydrogenative aminoacyloxylation of β,γ-unsaturated hydrazones with Togni reagent II is reported. Initiated by the carboxyl-containing species generated in situ from Togni reagent II, this method offers a new solution for regioselective functionalization at a remote site on β,γ-unsaturated hydrazones, thus providing a straightforward method for the synthesis of acyloxyl-substituted pyridazines. This reaction features a broad substrate scope and mild conditions.

Graphical abstract: PhI(OAc)2-mediated aminoacyloxylation of β,γ-unsaturated hydrazones using Togni reagent II as an acyloxyl precursor

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