Synfacts 2010(12): 1342-1342  
DOI: 10.1055/s-0030-1258959
Synthesis of Heterocycles
© Georg Thieme Verlag Stuttgart ˙ New York

Direct C2 Indole Trifluoromethylation Using Togni’s Reagent

Contributor(s): Victor Snieckus, Matthew O. Kitching
R. Shimizu, H. Egami, T. Nagi, J. Chae, Y. Hamashima, M. Sodeoka*
RIKEN, Advanced Science Institute, Saitama, Saitama University and Sodeoka Live Cell Chemistry Project, ERATO, Saitama, Japan
Further Information

Publication History

Publication Date:
22 November 2010 (online)

Significance

Reported is the trifluoromethylation of substituted indoles via copper catalysis employing Togni’s reagent as CF3 source. Solvent and catalyst screens are described. Indole C3 EWG substitution leads to lower yields of products; however, benzene ring substitution is well tolerated. N-Acyl indoles lead to inefficient transformations.