Copper-mediated C(sp2)–H amination using TMSN3 as a nitrogen source: redox-neutral access to primary anilines

Abstract

A Cu-mediated direct conversion of aromatic C–H to C–NH₂ assisted by a chelating group was developed. The reaction employed TMSN₃ as a nitrogen source under redox-neutral conditions to provide a variety of N-heterocycle-substituted primary anilines. Neither external oxidant nor additional deprotection or reduction step was required in this process.