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t‑BuOK-Mediated Oxidative Dehydrogenative C(sp3)‑H Arylation of 2‑Alkylazaarenes with Nitroarenes

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journal contribution
posted on 24.07.2017 by Shuai-Shuai Li, Shiheng Fu, Liang Wang, Lubin Xu, Jian Xiao
The first transition-metal free and regioselective C­(sp3)-H arylation of 2-alkylazaarenes with nitroarenes has been achieved via t-BuOK-mediated dehydrogenative C­(sp3)-C­(sp2) coupling. This reaction provides an efficient access to the biologically important and synthetically useful 2-benzyl-substituted azaarenes under mild conditions without the need of prefunctionalization of 2-alkylazaarenes or using the specialized arylating agents.