Assessing the Efficiency of ortho ‐Aminoaryl Carbonyls for Exploring Synthetic Diversity of Quinazolines: A Review

Abstract

Quinazoline‐based nitrogen heterocycles play vital role in medicinal chemistry due to their wide‐ranging biological activity and presence in several clinically relevant drugs and naturally occurring bioactive compounds. Beyond pharmaceuticals, quinazolines have applications in catalysis, materials science, sensing, supramolecular chemistry, and polymer science. Owing to their diverse adaptability, the significant advances have been made in the development of useful synthetic strategies for quinazolines, particularly ortho ‐aminoaryl carbonyl compounds such as 2‐aminoaryl aldehydes and ketones. This review provides a comprehensive and integrated overview of these synthetic methods, reaction pathways, substrate scope, functional group tolerance, and operational limitations. Emphasis is placed on 2‐aminoaryl aldehydes/ketones precursors facilitating metal‐catalyzed, metal‐free, and heterogeneous and sustainable one‐pot synthesis for quinazoline synthesis. The review offers useful insights for the coherent designing of diverse quinazolines and highlights prospects for next‐generation heterocyclic scaffolds.