Wang Shihui, Xu Jian, Song Qiuling
Institute of Next Generation Matter Transformation, College of Material Sciences Engineering at Huaqiao University, 668 Jimei Boulevard, Xiamen, Fujian 361021, China.
Guangdong Provincial Key Laboratory of Catalysis, Southern University of Science and Technology, Shenzhen 518055, Guangdong, China.
Org Lett. 2021 Sep 3;23(17):6789-6794. doi: 10.1021/acs.orglett.1c02373. Epub 2021 Aug 12.
Polysubstituted quinolin-3-amines are vital structural motifs because of their broad biological activities as well as versatile transformational abilities. However, they are not easily accessible. We disclose a protocol with Mn(III) acetate as a mild one-electron oxidant promoting a radical process to construct polysubstituted quinolin-3-amines. 2-(2-Isocyanophenyl)acetonitriles and organoboron reagents are suitable substrates for this reaction. The remarkable advantages of this protocol are the practical method, mild approach, high reaction efficiency, and good compatibility of functional groups, providing straightforward access to functional quinoline derivatives.
多取代喹啉-3-胺是重要的结构基序，因其具有广泛的生物活性以及多样的转化能力。然而，它们不易获得。我们公开了一种以醋酸锰(III)作为温和的单电子氧化剂促进自由基过程来构建多取代喹啉-3-胺的方法。2-(2-异氰基苯基)乙腈和有机硼试剂是该反应的合适底物。该方法的显著优点是方法实用、操作温和、反应效率高以及官能团兼容性好，为制备功能性喹啉衍生物提供了直接的途径。
