Cu(II)-Mediated Ortho-C–H Amination of Arenes with Free Amines

Copper-mediated direct ortho-C–H
amination of arenes has
been accomplished with the aid of easily removable bidentate pyridine N-oxide as a directing group. The use of free cyclic secondary
amines and anilines as aminating agents and inexpensive copper acetate
makes the strategy more effective and favorable from the economic
point of view. This reaction is compatible with a wide range of functional
groups to synthesize a variety of amine-containing products of high
interest. This method also allows the short synthesis of the central
scaffold of pharmaceutically relevant Staphylococcus
aureus Sortase A inhibitors.