Intramolecular C(sp3)–H amination

Increasing interest in C(sp3)–H bond functionalization has led to a multitude of recent advances in intramolecular C(sp3)–H amination. Direct, intramolecular C(sp3)–N bond-forming processes provide expedient access to a range of azacycles without the need for prefunctionalized amine precursors such as aminoaldehydes, aminoalkyl halides or aminoalkenes. Some of these methods have been successfully applied to the synthesis of complex natural products. This Perspective provides a historical context for these methods and describes recent contributions, as well as the remaining challenges to intramolecular C(sp3)–H amination.