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Updated: Sep 24, 2025

Protocol for the Synthesis of Ortho-trifluoromethoxylated Aniline Derivatives
Published on: January 19, 2016
An efficient 3-acylquinoline synthesis from acetophenones and anthranil via C(sp3)-H bond activation mediated by
Yejun Gao1,2, Robert C Hider3, Yongmin Ma1,2
1School of Pharmaceutical and Chemical Engineering, Taizhou University Taizhou 318000 PR China yongmin.ma@tzc.edu.cn.
Abstract:
An efficient method for the synthesis of 3-functionalized quinolines from commercially available acetophenones and anthranil has been described. Selectfluor propels the C(sp3)-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.
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