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无过渡金属参与的使用 Selectfluor 作为温和氧化剂的喹喔啉-2(1H)-酮的 C3-酰胺化反应。

Transition-metal free C3-amidation of quinoxalin-2(1H)-ones using Selectfluor as a mild oxidant.

机构信息

School of Chemistry & Chemical Engineering, Henan University of Technology; Academician Workstation for Natural Medicinal Chemistry of Henan Province, Zhengzhou 450001, China.

Henan Key Laboratory of Nanocomposites and Applications; Institute of Nanostructured Functional Materials, Huanghe Science and Technology College, Zhengzhou 450006, China.

出版信息

Org Biomol Chem. 2019 Dec 28;17(48):10178-10187. doi: 10.1039/c9ob02157d. Epub 2019 Nov 25.

Abstract

A practical and efficient synthetic route to construct a variety of 3-amidated quinoxalin-2(1H)-ones was developed via transition-metal free direct oxidative amidation of quinoxalin-2(1H)-ones with amidates using Selectfluor reagent as a mild oxidant. This protocol features mild reaction conditions, operational simplicity, broad substrate scope, and good to excellent yields.

摘要

开发了一种实用且高效的合成路线,通过使用 Selectfluor 试剂作为温和氧化剂,无需过渡金属即可实现喹喔啉-2(1H)-酮与酰胺基的直接氧化酰胺化,从而构建各种 3-酰胺基喹喔啉-2(1H)-酮。该方案具有温和的反应条件、操作简单、广泛的底物范围和良好至优秀的产率。

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