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Updated: Jun 7, 2025

Facile Preparation of 4-Substituted Quinazoline Derivatives
Published on: February 15, 2016
Organocatalytic Electrophilic Arene Amination: Rapid Synthesis of 2-Quinolones
Tamal Kanti Das1, Arghya Ghosh1, Zachary Grimm1
1Department of Chemistry, Rice University, Houston, Texas, 77030, USA.
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.
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