Ni Hangcheng, Shi Xingzi, Li Yu, Zhang Xiaoning, Zhao Jingwei, Zhao Fei
Jinhua Branch, Sichuan Industrial Institute of Antibiotics, Chengdu University, 888 West Hai Tang Road, Jinhua 321007, China.
Org Biomol Chem. 2020 Aug 26;18(33):6558-6563. doi: 10.1039/d0ob01423k.
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.
在热条件下，由碘苯二乙酸（PIDA）促进喹喔啉-2(1H)-酮与α-氧代羧酸进行直接的C3-H酰化反应，已以非常快的速度以中等至良好的产率实现。机理研究表明该反应通过自由基过程进行。此外，该方法可应用于克级反应和抗肿瘤剂的合成。这项工作代表了一种简单、方便且高效的合成3-酰化喹喔啉-2(1H)-酮的方法。
