Intramolecular functionalization of C(sp 3 ) H bonds adjacent to an amide nitrogen atom: Metal-free synthesis of 2-hydroxy-benzoxazinone derivatives
作者:Biao Gao、Kaili Chen、Xiaoling Bi、Jinxin Wang
DOI:10.1016/j.tet.2017.09.001
日期:2017.12
An intramolecular C(sp3)H bond functionalization adjacent to an amide nitrogen atom was successfully developed for synthesis of 2-hydroxybenzoxazinone derivatives under environment-friendly conditions. The method featured no metal catalyst, broad substrate scopes and high yields. Besides, a radical mechanism was proposed in the reaction process. Additionally, most of target compounds exhibited potent
一个分子内的C(sp 3)H键功能与酰胺氮原子相邻已成功开发了在环境友好的条件下合成2-羟基苯并恶嗪酮衍生物。该方法无金属催化剂,底物范围宽,收率高。此外,在反应过程中还提出了自由基机理。另外,大多数目标化合物对MCF-7和Hela细胞表现出有效的抗增殖活性。