One-pot synthesis of 1-(trifluoromethyl)-4-fluoro-1,2-dihydroisoquinolines and 4,4-difluoro-1,2,3,4-tetrahydroisoquinolines.

A cascade approach to 1-(trifluoromethyl)-4-fluoro-1,2-dihydroisoquinolines and 4,4-difluorotetrahydroisoquinolines has been developed. The procedure involves a silver-catalyzed intramolecular aminofluorination of alkyne. This one-pot reaction provides an efficient way to synthesize various fluorinated isoquinolines.