Facile Assembly of Fused Isoquinolines by Gold(I)‐Catalyzed Coupling–Cyclization Reactions between o‐Alkynylbenzaldehydes and Aromatic Amines Containing Tethered Nucleophiles

A gold(I)‐catalyzed, operationally simple coupling–cyclization technique was developed for the synthesis of isoquinoline‐fused polycyclic compounds. The reaction makes use of two coupling partners such as o‐alkynylbenzaldehydes and aromatic amines having tethered nucleophiles. The reaction is easy to perform, broad in scope, and allows the generation of a number of biologically important heterocyclic motifs from readily accessible starting materials. A mechanism for the reaction is discussed.