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

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

The Journal of organic chemistry (2011-09-09)
Xiaohu Deng, Armin Roessler, Ivana Brdar, Roger Faessler, Jiejun Wu, Zachary S Sales, Neelakandha S Mani
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.