Organocatalytic Electrophilic Arene Amination: Rapid Synthesis of 2‐Quinolones

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.