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

The Cu-mediated N-H trifluoroethylation of NH-containing heteroaromatic compounds with the CF3CHCl2 (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.

Automated summary

The Cu-mediated N-H trifluoroethylation of NH-containing heteroaromatic compounds with CF3CHCl2 (HCFC-123) has been achieved, which is commercially available in industrial scale. This method is applicable to various NH-containing heteroaromatic compounds, including indoles, pyrroles, pyrazoles, and carbazoles. Moreover, this protocol enables the late-stage trifluoroethylation of NH-containing heteroaromatic bioactive molecules.