Journal
ORGANIC LETTERS
Volume 24, Issue 9, Pages 1859-1864Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acs.orglett.2c00454
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Funding
- Nature Science Foundation of China [22167011, 22061013]
- Guangxi Natural Science Fundation [2018GXNSFAA281203, 2020GXNSFAA297227]
- Guangxi Science and Technology Base and Special Fund for Talents [AD19245008, AD19110110]
- Key Laboratory of Electrochemical and Magnetochemical Function Materials [EMFM20211123]
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With control by N1-substituents, switchable divergent C-H functionalization reaction of quinoxalin-2(1H)-ones was achieved for the synthesis of (Z)-enaminones and furo[2,3-b]quinoxalines using copper catalyst and oxidant. The method features mild reaction conditions, readily available materials, and a broad substrate scope, and the desired products showed excellent antitumor activity against A549, HepG-2, MCF-7, and HeLa cells.
With control by N1-substituents, the switchable divergent C-H functionalization reaction of quinoxalin-2(1H)-ones is achieved for the synthesis of (Z)-enaminones and furo[2,3-b]quinoxalines using the combination of a copper catalyst and an oxidant. This new protocol features mild reaction conditions, readily available materials, and a broad substrate scope. Gram-scale and mechanistic studies were also investigated. Furthermore, the desired products exhibited excellent antitumor activity against A549, HepG-2, MCF-7, and HeLa cells, which were tested by MTT assay.
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