Metal-free C3–H acylation of quinoxalin-2(1<i>H</i>)-ones with α-oxo-carboxylic acids
Hangcheng Ni, Xingzi Shi, Yu Li, Xiaoning Zhang, Jingwei Zhao, Fei Zhao
Abstract
Direct C3-H acylation of quinoxalin-2(1H)-ones with α-oxocarboxylic acids under thermo conditions promoted by PIDA has been achieved in a moderate to good yield in a very fast manner. Mechanistic study revealed that the reaction proceeds via a radical process. In addition, this method could be applied to a gram-scale reaction and antitumor agent synthesis. This work represents a simple, convenient and efficient synthesis of 3-acylated quinoxalin-2(1H)-ones.
Topics & Concepts
ChemistryAcylationYield (engineering)Combinatorial chemistryMetalOrganic chemistryCatalysisMaterials scienceMetallurgySynthesis and Biological EvaluationCatalytic C–H Functionalization MethodsRadical Photochemical Reactions