Synfacts 2005(1): 0113-0113  
DOI: 10.1055/s-2005-872200
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart · New York

Palladium-Catalyzed Regioselective Direct C-2 and C-3 Functionalization of Indoles

Contributor(s): Victor Snieckus, Oleg M. Demchuk
N. P. Grimster, C. Gauntlett, C. R. A. Godfrey, M. J. Gaunt*
University of Cambridge, UK and Syngenta Crop Protection Research AG, Basel, Switzerland
Further Information

Publication History

Publication Date:
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.).