Description:
A highly efficient synthesis of [1,2,3]triazolo[5,1‐a]isoquinoline derivatives was developed that proceeds through copper‐catalyzed tandem Sonogashira coupling/regioselective 6‐endo cyclization. This NH‐triazole‐directed annulation approach showed good functional‐group tolerance and gave the corresponding N‐fused heterocycles in good to excellent yields.