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. 2011 Oct 21;76(20):8262-9.
doi: 10.1021/jo201425q. Epub 2011 Sep 7.

Direct, metal-free amination of heterocyclic amides/ureas with NH-heterocycles and N-substituted anilines in POCl3

Xiaohu Deng  1 , Armin Roessler, Ivana Brdar, Roger Faessler, Jiejun Wu, Zachary S Sales, Neelakandha S Mani
Affiliations

Direct, metal-free amination of heterocyclic amides/ureas with NH-heterocycles and N-substituted anilines in POCl3

Xiaohu Deng et al. J Org Chem. .

Abstract

A POCl(3)-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.

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