Facile Synthesis of [1,2,3]Triazolo[5,1‐<i>a</i>]isoquinolines through a Copper‐Catalyzed Tandem Sonogashira Coupling/Cyclization Reaction

Abstract

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.