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