Lewis Acid–Catalyzed Annulation of 2(Trifluoroacetyl)pyrroles Leading to CF3-Substituted Polycyclic Quinazolinones

Abstract

A novel and efficient cascade annulation of 2-aminobenzamides with N-aryl 2-(trifluoroacetyl)pyrroles has been developed, providing a straightforward route to CF ₃ -substituted quinazolinones. The reaction proceeds smoothly under mild conditions via a dehydrative annulation pathway, enabling the formation of a C–N bond in a single operation. This transformation effectively incorporates the trifluoromethyl group into the quinazolinone framework, affording structurally diverse CF ₃ -substituted quinazolinones in good to excellent yields. This methodology provides a practical approach for the synthesis of fluorine-containing heterocycles of potential pharmaceutical interest.