Synthesis of spiroindolenine-3,3'-pyrrolo[2,1- b ]quinazolinones through gold(I)-catalyzed dearomative cyclization of N -alkynyl quinazolinone-tethered indoles.

A variety of functionalized spiroindolenine-3,3'-pyrrolo[2,1- b ]quinazolinones were prepared in good to excellent yields through a gold(I)-catalyzed dearomative cyclization of N -alkynyl quinazolinone-tethered C2-substituted indoles. This reaction features a broad substrate scope, good functional group tolerance, and easy gram-scale preparation and transformations. Furthermore, biological activity studies showed that most of the obtained spiroindolenine-3,3'-pyrrolo[2,1- b ]quinazolinone scaffolds showed potential as good anti-inflammatory agents.