A practical and efficient approach to imidazo[1,2-]pyridine-fused isoquinolines through the post-GBB transformation strategy.

Diversity-oriented synthesis of the biologically intriguing imidazo[1,2-]pyridine-fused isoquinoline systems from readily available starting materials was achieved through the Groebke-Blackburn-Bienaymé reaction followed by a gold-catalyzed cyclization strategy. The synthetic approach is characterized by mild reaction conditions and a broad substrate scope, allowing for the rapid construction of structurally complex and diverse heterocycles in moderate to good yields.