Metal-free (Boc)2O-mediated C4-selective direct indolation of pyridines using TEMPO?

Organic & Biomolecular Chemistry Pub Date: 2014-04-22 DOI: 10.1039/C4OB00356J

Abstract

Direct metal-free C-4-selective indolation of pyridines is achieved for the first time using TEMPO and (Boc)2O. A variety of substituents on both indoles and pyridines are tolerated to give 3-(pyridin-4-yl)-1H-indole derivatives in moderate to excellent yields. This finding provides a novel approach for developing metal-free C–H functionalization of pyridines.

Graphical abstract: Metal-free (Boc)2O-mediated C4-selective direct indolation of pyridines using TEMPO
Recommended Literature