Synthesis of 2-(Trifluoromethyl)-[1,2,4]triazolo[5,1- a ]isoquinoline via Cycloaddition of C , N -Cyclic Azomethine Imine with CF 3 CN.

A [3 + 2] cycloaddition of C , N -cyclic azomethine imine with in situ-generated CF 3 CN for the construction of 2-(trifluoromethyl)-[1,2,4]triazolo[5,1- a ]isoquinoline is reported. Remarkably, this process shows a broad substrate scope with excellent functional group tolerance, which is scalable and enables a practical route to a library of 2-(trifluoromethyl)-[1,2,4]triazolo[5,1- a ]isoquinoline derivatives in moderate to good yields.