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Unveiling the reaction process of the amine in direct amidation of aromatic ketones in H2O
Authors:Dr Fangjun He  Dr Rumeng Qu  Dr Jie Su  Muyao Du  Dr Junqiang Liu  Yiping Chen  Prof Bo Wang
Institution:1. Key Laboratory of Advanced Materials of Tropical Island Resources(Hainan University), Ministry of Education, Hainan University, No. 58, Renmin AVE, Haikou, 570228 China

Both authors contributed equally to this work.;2. Key Laboratory of Advanced Materials of Tropical Island Resources(Hainan University), Ministry of Education, Hainan University, No. 58, Renmin AVE, Haikou, 570228 China;3. School of Food Science, Shandong Agricultural University, No. 61, Daizhong AVE, Taian, 271018 China

Abstract: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.
Keywords:amidation reaction  aromatic ketones  α-ketoamide  reaction mechanism  NMR spectroscopy
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