Experimental study demonstrates transition-metal-free C(sp3)-H arylation of 2-alkylazaarenes with nitroarenes, providing an efficient route to bioactive 2-benzylazaarenes under mild conditions.
The first transition-metal free and regioselective C(sp 3 )-H arylation of 2-alkylazaarenes with nitroarenes has been achieved via t -BuOK-mediated dehydrogenative C(sp 3 )-C(sp 2 ) 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.
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Li et al. (2017) studied this question.
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