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Copper-Catalyzed Direct Amination of Quinoline N‑Oxides via C–H Bond Activation under Mild Conditions

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journal contribution
posted on 04.04.2014, 00:00 by Chongwei Zhu, Meiling Yi, Donghui Wei, Xuan Chen, Yangjie Wu, Xiuling Cui
A highly efficient and concise one-pot strategy for the direct amination of quinoline N-oxides via copper-catalyzed dehydrogenative C–N coupling has been developed. The desired products were obtained in good to excellent yields for 22 examples starting from the parent aliphatic amines. This methodology provides a practical pathway to 2-aminoquinolines and features a simple system, high efficiency, environmental friendliness, low reaction temperature, and ligand, additives, base, and external oxidant free conditions.