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

J Org Chem. 2017 Aug 18;82(16):8703-8709. doi: 10.1021/acs.joc.7b00732. Epub 2017 Aug 1.

Abstract

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.

Publication types

  • Research Support, Non-U.S. Gov't