Bradley Robert D, Bahamonde Ana
Department of Chemistry, University of California, Riverside, California 92521, United States.
Org Lett. 2022 Oct 7;24(39):7134-7139. doi: 10.1021/acs.orglett.2c02808. Epub 2022 Sep 26.
This paper describes a mild strategy to promote amide arylations. Photoinduced oxidation of a Ni(II) aryl amido intermediate is proposed to facilitate the challenging C-N reductive elimination step at moderate temperatures. Notably, the mildly basic conditions employed facilitate access to a broad scope including protected amino acids, heterocycles, phenols, and sterically hindered substituents. Hence, this work presents an attractive strategy to enable late-stage functionalization of pre-existing amide moieties in commercial drugs and natural products.
本文描述了一种促进酰胺芳基化的温和策略。有人提出，光诱导氧化镍（II）芳基酰胺中间体有助于在中等温度下实现具有挑战性的C-N还原消除步骤。值得注意的是，所采用的温和碱性条件有助于获得广泛的底物范围，包括受保护的氨基酸、杂环、酚类和空间位阻取代基。因此，这项工作提出了一种有吸引力的策略，能够实现市售药物和天然产物中已有酰胺部分的后期功能化。
