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

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.