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

Diversity-oriented synthesis of the biologically intriguing imidazo[1,2-a]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.

One-pot synthesis of tetracyclic fused imidazo[1,2-a]pyridines via a three-component reaction.

A novel three-component reaction has been developed to assemble biologically and pharmaceutically important tetracyclic fused imidazo[1,2-a]pyridines in a one-pot fashion utilizing readily available 2-aminopyridines, isatins and isocyanides. The three-component coupling proceeds through the Groebke-Blackburn-Bienaymé reaction followed by a retro-aza-ene reaction and subsequent nucleophilic reaction of the in-situ generated imidazo[1,2-a]pyridines bearing an isocyanate functional group.

Syntheses of fused tetracyclic quinolines via Ugi-variant MCR and Pd-catalyzed bis-annulation.

Diversity-oriented synthesis of fused tetracyclic 6,11-dihydroquinoxalino[2,3-b]quinolines is described via a sequential Ugi-variant multicomponent reaction and Pd-catalyzed bis-annulation in one-pot process.

Synthesis and characterization of Sant-75 derivatives as Hedgehog-pathway inhibitors.

Sant-75 is a newly identified potent inhibitor of the hedgehog pathway. We designed a diversity-oriented synthesis program, and synthesized a series of Sant-75 analogues, which lays the foundation for further investigation of the structure-activity relationship of this important class of hedgehog-pathway inhibitors.