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Intramolecular functionalization of C(sp3)H bonds adjacent to an amide nitrogen atom: Metal-free synthesis of 2-hydroxy-benzoxazinone derivatives
Tetrahedron ( IF 2.1 ) Pub Date : 2017-09-06 , DOI: 10.1016/j.tet.2017.09.001
Biao Gao , Kaili Chen , Xiaoling Bi , Jinxin Wang

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 anti-proliferative activities against MCF-7 and Hela cells.



中文翻译:

与酰胺氮原子相邻的C(sp 3H键的分子内官能化:2-羟基-苯并恶嗪酮衍生物的无金属合成

一个分子内的C(sp 3H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。

更新日期:2017-09-06
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