Visible-Light-Mediated Skeletal Editing of Furans to N -Aminopyrroles

Abstract N-Aminopyrroles are privileged scaffolds in pharmaceuticals, agrochemicals, and bioactive natural products. Despite some advances in their synthesis, general and efficient routes to these motifs remain underexplored. Herein, we report a visible-light-driven skeletal rearrangement of furans to N-aminopyrroles using Boc-hydrazine as the nitrogen source at room temperature, enabling efficient O-to-N atom exchange on the furan ring. The method accommodates a broad range of aryl-substituted furans and complex natural product derivatives, providing 31 examples with yields of up to 98%. This mild protocol offers practical access to functionalized N-aminopyrroles from furans and holds promise for medicinal chemistry and late-stage natural product functionalization.