通过Selectfluor介导的苯乙酮和邻氨基苯甲酸C(sp) - H键活化高效合成3 - 酰基喹啉。
An efficient 3-acylquinoline synthesis from acetophenones and anthranil C(sp)-H bond activation mediated by Selectfluor.
作者信息
Gao Yejun, Hider Robert C, Ma Yongmin
机构信息
School of Pharmaceutical and Chemical Engineering, Taizhou University Taizhou 318000 PR China
School of Pharmaceutical Science, Zhejiang Chinese Medical University Hangzhou 310053 PR China.
出版信息
RSC Adv. 2019 Apr 2;9(18):10340-10344. doi: 10.1039/c9ra01481k. eCollection 2019 Mar 28.
An efficient method for the synthesis of 3-functionalized quinolines from commercially available acetophenones and anthranil has been described. Selectfluor propels the C(sp)-H bond activation of the acetophenones and aza-Michael addition of anthranil resulting in annulated 3-acylquinolines in moderate to high yields. DMSO acts not only as a solvent but also as a one carbon donor in the reaction.
已描述了一种从市售苯乙酮和邻氨基苯甲酸合成3-官能化喹啉的有效方法。Selectfluor推动苯乙酮的C(sp)-H键活化以及邻氨基苯甲酸的氮杂迈克尔加成反应，从而以中等至高收率得到稠合的3-酰基喹啉。二甲基亚砜在反应中不仅作为溶剂，还作为一碳供体。
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