Find in Library

A consecutive 2-step synthesis of <i>N</i>-unprotected polysubstituted indoles bearing an electron-withdrawing group at the C-3 position from readily available nitroarenes is reported. The protocol is based on the [3,3]-sigmatropic rearrangement of <i>N</i>-oxyenamines generated by the DABCO-catalyzed reaction of <i>N</i>-arylhydroxylamines and conjugated terminal alkynes, and delivers indoles endowed with a wide array of substitution patterns and topologies.