Pd/C as an efficient heterogeneous catalyst for carbonylative four-component synthesis of 4(3H)-quinazolinones

Quinazolinones are of interest in the fields of pharmaceuticals and medicinal chemistry. The application of palladium on activated charcoal (Pd/C) as a heterogeneous catalyst was investigated for the carbonylation of 2-iodoanilines with trimethyl orthoformate and amines via a multicomponent reaction approach, which provided excellent yields of 4(3H)-quinazolinones. It avoids the use of expensive phosphine ligands with an additional advantage of catalyst recovery. Furthermore, >5 new quinazolinone scaffolds containing the trifluoroethyl group were introduced by this procedure; gram scale experiments were successfully performed as well.