Exploring Synthetic Approaches for 2‐Aminoquinolines: Progress and Future Directions

Abstract This review article presents a thorough overview of recent advancements in the synthesis of 2‐aminoquinolines, a vital class of N ‐heterocyclic aromatic compounds with significant biological and pharmaceutical relevance. It systematically summarizes the progress made from early 2019 to the end of 2024, categorizing synthetic approaches into three main types: cyclization of C2‐substituted anilines and related compounds, amination of nitroxides, 2‐haloquinolines, 2‐quinolones, and quinolines, and ring‐opening cyclization of heteroaryl amines and their derivatives. The discussion includes various methods such as metal‐catalyzed reactions, organocatalysis, and redox‐neutral processes, highlighting their advantages regarding reaction conditions, substrate scope, and yields. Additionally, the review addresses current challenges and future directions, emphasizing the need for more sustainable and efficient synthetic strategies. This compilation serves as a valuable reference for researchers aiming to develop novel 2‐aminoquinoline derivatives with potential applications in pharmaceuticals and materials science.