Direct, Metal-Free Amination of Heterocyclic Amides/Ureas with NH-Heterocycles and N-Substituted Anilines in POCl3

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• 作者：Xiaohu Deng ; Armin Roessler ; Ivana Brdar ; Roger Faessler ; Jiejun Wu ; Zachary S. Sales ; Neelakandha S. Mani
• 刊名：Journal of Organic Chemistry
• 出版年：2011
• 出版时间：October 21, 2011
• 年：2011
• 卷：76
• 期：20
• 页码：8262-8269
• 全文大小：1064K
• 年卷期：v.76,no.20(October 21, 2011)
• ISSN：1520-6904

文摘

A POCl₃-mediated, direct amination reaction of heterocyclic amides/ureas with NH-heterocycles or N-substituted anilines is described. Compared to the existing methods, this operationally simple protocol provides unique reactivity and functional group compatibility because of the metal-free, acidic reaction conditions. The yields are generally excellent.