Base-promoted [3+2] cycloaddition/aromatization cascade reaction under air: An approach to access perfluoroalkylated pyrrolo [2,1-a] isoquinolines

A facile [3 + 2] cycloaddition / aromatization cascade reaction with broad substrate scopes in up to 94% isolated yield was disclosed herein. This tandem approach was accomplished by employing isoquinolines and bromoacetyl derivatives with methyl perfluoroalk-2-ynoates as readily available starting materials. In the presence of base, this method provides an efficient access to synthesize perfluoroalkylated pyrrolo[2,1-a]isoquinolines with ambient air as a terminal oxidant at room temperature in one-pot.