三氯氧磷中杂环酰胺/脲与 NH-杂环和 N-取代苯胺的直接、无金属氨化反应。
Direct, metal-free amination of heterocyclic amides/ureas with NH-heterocycles and N-substituted anilines in POCl3.
机构信息
Johnson & Johnson Pharmaceutical Research & Development, LLC, 3210 Merryfield Row, San Diego, California 92121, United States.
出版信息
J Org Chem. 2011 Oct 21;76(20):8262-9. doi: 10.1021/jo201425q. Epub 2011 Sep 7.
PMID:21899258
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.
摘要
本文描述了一种 POCl(3)介导的杂环酰胺/脲与 NH-杂环或 N-取代苯胺的直接胺化反应。与现有方法相比，由于无金属、酸性反应条件，这种操作简单的方案提供了独特的反应性和官能团兼容性。产率通常很高。
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