5 years ago

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

t-BuOK-Mediated Oxidative Dehydrogenative C(sp3)-H Arylation of 2-Alkylazaarenes with Nitroarenes
Lubin Xu, Shuai-Shuai Li, Jian Xiao, Liang Wang, Shiheng Fu
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.

Publisher URL: http://dx.doi.org/10.1021/acs.joc.7b00732

DOI: 10.1021/acs.joc.7b00732

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