N−H Trifluoroethylation of Indoles and other Aromatic N‐Heterocycles with CF₃CHCl₂ by Copper‐Mediated Cross‐Coupling Reaction

Abstract The Cu‐mediated N−H trifluoroethylation of NH‐containing heteroaromatic compounds with the CF 3 CHCl 2 (HCFC‐123), commercially available in industrial scale, has been achieved. This method can be applied to various NH‐containing heteroaromatic compounds including indoles, pyrroles, pyrazoles and carbazoles. Furthermore, this protocol allows the late‐stage trifluoroethylation of NH‐containing heteroaromatic bioactive‐molecules. magnified image