3 years ago

Regioselective and Direct Azidation of Anilines via Cu(II)-Catalyzed C–H Functionalization in Water

Regioselective and Direct Azidation of Anilines via Cu(II)-Catalyzed C–H Functionalization in Water
Yuguo Zheng, Mohit Chhabra, Hongli Fang, Yandong Dou, Pengfei Zhang, Jingyan Ge, Qing Zhu, Hongyan Sun
We report herein the first example of Cu(II)-catalyzed site selective azidation of aromatic amines via C–H functionalization in aqueous media. In our strategy, a mild reagent was utilized. H2O2 served as the oxidant, and sodium azide was used as the azidation reagent. This method could also be applied to late-stage functionalization of drugs that possess an aromatic amine moiety. In addition, we found that bromination or iodination on the ortho-position of aromatic amines could occur efficiently using this catalytic system.

Publisher URL: http://dx.doi.org/10.1021/acs.joc.7b01594

DOI: 10.1021/acs.joc.7b01594

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