Here we report a method for the site-selective intermolecular C­(sp3)–H amination of carboxamides by merging transition-metal catalysis and the hydrogen atom transfer strategy. The reaction proceeds through a sequence of favorable single-electron transfer, 1,5-hydrogen atom transfer, and C–N cross-coupling steps, thus allowing access to a series of desired products. This reaction could accommodate a wide diversity of nitrogen nucleophiles as well as demonstrate excellent chemoselectivity and functional group compatibility.

A mild and practical protocol is developed for the synthesis of distal azido and thiocyanato alkylamines via N-directed remote C(sp3)–H functionalization.

No abstract