Rh(III)-Catalyzed Intermolecular C–H Amination of 1-Aryl-1H-pyrazol-5(4H)-ones with Alkylamines

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• 作者：Kui Wu ; Zhoulong Fan ; Yu Xue ; Qizheng Yao ; Ao Zhang
• 刊名：Organic Letters
• 出版年：2014
• 出版时间：January 3, 2014
• 年：2014
• 卷：16
• 期：1
• 页码：42-45
• 全文大小：346K
• ISSN：1523-7052

文摘

An intermolecular C鈥揌 amination of 1-aryl-1H-pyrazol-5(4H)-ones was achieved under mild reaction conditions, using a low catalyst loading and with a broad scope of aminating reagents. This protocol not only provides the first example of rhodium(III)-catalyzed intermolecular aromatic C鈥揌 amination directed by an intrinsic functionality of the substrate/product but also features aminating an existing drug with either primary or secondary N-benzoate alkylamines as the coupling partners.