Intermolecular Amination of Unactivated C(sp³)−H Bonds with Cyclic Alkylamines: Formation of C(sp³)−N Bonds through Copper/Oxygen‐Mediated C(sp³)−H/N−H Activation

Abstract

The first example of intermolecular amination of unactivated C(sp³ )-H bonds by cyclic alkylamines mediated by Cu(OAc)₂ /O₂ is reported. This method avoids the use of benzoyloxyamines as the aminating reagent, which are normally prepared from alkylamines in extra steps. A variety of unnatural β^{2, 2} -amino acid analogues are synthesized by this simple and efficient procedure. This approach offers a solution to the previous unmet challenge of C(sp³ )-H/N-H activation for the formation of C(sp³ )-N bonds.