Palladium-Catalyzed Regioselective Direct C-2 and C-3 Functionalization of Indoles
N. P. Grimster, C. Gauntlett, C. R. A. Godfrey, M. J. Gaunt*
University of Cambridge, UK and Syngenta Crop Protection Research AG, Basel, Switzerland
21 September 2005 (online)
New methods for direct regioselective C-3 and C-2 functionalization of indoles by combined C-H activation-oxidative Heck processes are reported. The reactions proceed under mild conditions, in good to excellent yields, and show a reasonably broad scope typical of Heck reactions (For independent and concurrent work concerning regioselective C-3 and C-2 direct arylation of azoles, see B. S. Lane, M. A. Brown, D. Sames J. Am. Chem. Soc. 2005, 127, 8050-8057.).