Organocatalytic Electrophilic Arene Amination: Rapid Synthesis of 2‐Quinolones

Abstract

For decades, the synthesis of 2‐quinolones, a crucial structural motif in pharmaceuticals and agrochemicals, has relied heavily on costly noble metal complexes and structurally complex ligands. Despite considerable efforts from synthetic chemists, a mild, metal‐free, environmentally friendly, and cost‐effective approach has remained elusive. This study introduces a robust, metal‐free synthetic platform that leverages an innovative organoiodine‐catalyzed electrophilic arene C(sp2)‐H amination strategy to efficiently produce a wide range of new and modifiable 2‐quinolones. Moreover, this study allows ready synthetic access to novel 8‐aryl‐substituted 2‐quinolones, uncovering new chemical spaces with significant potential for medicinal applications.