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使用钌催化剂实现苯胺衍生物与α-氧代羧酸的 C-H 酰化反应。

C-H acylation of aniline derivatives with α-oxocarboxylic acids using ruthenium catalyst.

机构信息

School of Chemical and Biological Engineering, University of Science and Technology Beijing, Beijing 100083, China.

Institute of Chinese Materia Medica, China Academy of Chinese Medical Sciences, Beijing 100700, P. R. China.

出版信息

Org Biomol Chem. 2022 Aug 31;20(34):6890-6896. doi: 10.1039/d2ob01212j.

Abstract

An efficient and convenient synthetic strategy for ruthenium(II)-catalyzed -acylation of -(2-pyridyl)-anilines using α-oxycarboxylic acids as acyl sources is described. The procedure can smoothly proceed under mild conditions, showing good functional group tolerance. Valuable -acylated aniline products have been obtained with moderate to good yields. Furthermore, the reaction could be easily scaled up to the gram scale.

摘要

描述了一种使用α-氧羧酸作为酰基源,通过钌(II)催化的-酰化-(2-吡啶基)苯胺的高效、便捷的合成策略。该反应在温和的条件下能顺利进行,对官能团具有良好的耐受性。得到了具有中等至良好收率的有价值的-酰化苯胺产物。此外,该反应可轻松放大至克级规模。

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