2-(Trifluoromethyl)indoles via Pd(0)-Catalyzed C(sp(3))-H Functionalization of Trifluoroacetimidoyl Chlorides
Perfluoroalkylated indoles are valuable compounds in drug discovery. A Pd(0)-catalyzed C(sp(3))-H functionalization enables access to 2-(trifluoromethyl)indoles from trifluoroacetimidoyl chlorides. These are stable compounds, easily obtained from anilines. The cyclization operates with catalyst loadings as low as 1 mol % and accommodates a variety of substituents.