Facile Entry to Pharmaceutically Important 3-Difluoromethyl-quinoxalin-2-ones Enabled by Visible-Light-Driven Difluoromethylation of Quinoxalin-2-ones
CF<sub>2</sub>H moiety has a significant potential utility in drug design and discovery, and the incorporation of CF<sub>2</sub>H into biologically active molecules represents an important and efficient strategy for seeking lead compounds and drug candidates. On the other han...
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| Main Authors: | , , , , |
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| Format: | Book |
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MDPI AG,
2022-12-01T00:00:00Z.
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| Online Access: | Connect to this object online. |
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| Summary: | CF<sub>2</sub>H moiety has a significant potential utility in drug design and discovery, and the incorporation of CF<sub>2</sub>H into biologically active molecules represents an important and efficient strategy for seeking lead compounds and drug candidates. On the other hand, quinoxalin-2-one is of great interest to pharmaceutical chemists as a common skeleton frequently occurring in plenty of natural products and bioactive compounds. Herein, we reported a practical and efficient protocol for the synthesis of 3-CF<sub>2</sub>H-quinoxalin-2-ones. Thus, in the presence of 3 mol% of photocatalyst and <i>S</i>-(difluoromethyl)sulfonium salt as difluoromethyl radical sources, a wide range of quinoxalin-2-ones readily underwent a visible-light redox-catalyzed difluoromethylation reaction, to deliver structurally diverse 3-difluoromethyl-quinoxalin-2-ones. We believe that this would facilitate increasing chances and possibilities for seeking potential lead compounds and drug candidates and further boost the development of fluorine-containing pharmaceuticals. |
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| Item Description: | 10.3390/ph15121552 1424-8247 |