Copper-catalyzed amidation of Sp3 C-H bonds adjacent to a nitrogen atom

We have developed a novel copper-catalyzed amidation of unactivated sp(3) C-H bonds adjacent to a nitrogen atom by using an inexpensive catalyst-oxidant (CuBr/(BuOOH)-Bu-t) system under mild conditions. The dephenylation was first found for N-benzylaniline, and the new class of products provide diverse structures for pharmaceuticals and combinatorial chemistry.