Ru-Jian Yu, Chun-Yan Zhang, Xiang Zhou, Xiong Yan-Shi, Duan Xue-Min
Jiangxi Provincial Key Laboratory of Drug Design and Evaluation, School of Pharmacy, Jiangxi Science & Technology Normal University, Nanchang, 330013, Jiangxi, P. R.China.
Org Biomol Chem. 2021 Apr 7;19(13):2901-2906. doi: 10.1039/d1ob00106j. Epub 2021 Mar 16.
A copper-catalyzed direct C-H chalcogenation of N-aryl-azaindoles with disulfides is described. This transformation was performed using Earth abundant Cu(OAc) as a catalyst, benzoic acid as an additive, air as a terminal oxidant, and readily available diaryl and dialkyldisulfides (or diselenide) as chalcogenation reagents. High functional group tolerance and excellent regioselectivity are demonstrated by the efficient preparation of a wide range of ortho-sulfenylation-7-azaindoles.
