Synthesis of 2-(Trifluoromethyl)-[1,2,4]triazolo[5,1-]isoquinoline via Cycloaddition of ,-Cyclic Azomethine Imine with CFCN.

A [3 + 2] cycloaddition of ,-cyclic azomethine imine with in situ-generated CFCN for the construction of 2-(trifluoromethyl)-[1,2,4]triazolo[5,1-]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-]isoquinoline derivatives in moderate to good yields.