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Unveiling the reaction process of the amine in direct amidation of aromatic ketones in H2O
ChemistryOpen ( IF 2.3 ) Pub Date : 2020-10-07 , DOI: 10.1002/open.202000178
Fangjun He 1 , Rumeng Qu 1 , Jie Su 1 , Muyao Du 2 , Junqiang Liu 1 , Yiping Chen 1 , Bo Wang 1, 3
Affiliation  

In the classical amidation between aromatic ketones and amines, 2.0 equivalents of amines are necessarily required to gain satisfying yields. The specific role of the amine in the direct amidation already puzzled us for a long time. In this work, we disclosed that the amine acts as both reactant and catalyst. Specifically, the determination of reaction intermediates revealed the full mechanism, based on which, the introduction of one equivalent base in the amidation is showcased here that a high yield (∼95 %) can be afforded using only 1.1 equiv. of amine.

中文翻译:

揭示胺在H2O中直接酰胺化芳香酮的反应过程

在芳香酮和胺之间的经典酰胺化中,必须需要 2.0 当量的胺才能获得令人满意的产率。胺在直接酰胺化中的具体作用已经让我们困惑了很长时间。在这项工作中,我们公开了胺既可以作为反应物,也可以作为催化剂。具体来说,反应中间体的测定揭示了完整的机理,基于此,此处展示了在酰胺化中引入一个当量碱,仅使用 1.1 equiv 即可提供高产率(~95%)。的胺。
更新日期:2020-10-07
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