Lewis Acid–Catalyzed Annulation of 2(Trifluoroacetyl)pyrroles Leading to <scp> CF ₃ </scp> ‐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.