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. 2014 Mar 5;136(9):3354-7.
doi: 10.1021/ja412880r. Epub 2014 Feb 25.

Cu(II)-mediated C-H amidation and amination of arenes: exceptional compatibility with heterocycles

Ming Shang  1 , Shang-Zheng Sun, Hui-Xiong Dai, Jin-Quan Yu
Affiliations

Cu(II)-mediated C-H amidation and amination of arenes: exceptional compatibility with heterocycles

Ming Shang et al. J Am Chem Soc. .

Abstract

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.

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