Intermolecular Radical C(sp3)-H Amination under Iodine Catalysis

The direct amination of aliphatic C-H bonds has remained one of the most tantalizing transformations in organic chemistry. Herein, we report on a unique catalyst system, which enables the elusive intermolecular C(sp(3))-H amination. This practical synthetic strategy provides access to aminated building blocks and fosters innovative multiple C-H amination within a new approach to aminated heterocycles. The synthetic utility is demonstrated by the synthesis of four relevant pharmaceuticals.