Cu(II)-Mediated C–H Amidation and Amination of Arenes: Exceptional Compatibility with Heterocycles

A Cu­(OAc)2-mediated C–H amidation and amination of arenes and heteroarenes has been developed using a readily removable directing group. A wide range of sulfonamides, amides, and anilines function as amine donors in this reaction. Heterocycles present in both reactants are tolerated, making this a broadly applicable method for the synthesis of a family of inhibitors including 2-benzamidobenzoic acids and N-phenylaminobenzoates.