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.

Automated summary

In this study, functionalized spiroindolenine-3,3'-pyrrolo[2,1-b]quinazolinones with good anti-inflammatory activity were synthesized through a gold(I)-catalyzed reaction. The reaction showed a broad substrate scope and easy scalability.