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...
Saved in:
Main Authors: | , , , , |
---|---|
Format: | Book |
Published: |
MDPI AG,
2022-12-01T00:00:00Z.
|
Subjects: | |
Online Access: | Connect to this object online. |
Tags: |
Add Tag
No Tags, Be the first to tag this record!
|
MARC
LEADER | 00000 am a22000003u 4500 | ||
---|---|---|---|
001 | doaj_f4b39e4bd6564fe2b53f6c1407b2e32c | ||
042 | |a dc | ||
100 | 1 | 0 | |a Kai-Zhong Fu |e author |
700 | 1 | 0 | |a Xu-Xin Chen |e author |
700 | 1 | 0 | |a Ya-Shi Zhao |e author |
700 | 1 | 0 | |a Yuan-Qing Gu |e author |
700 | 1 | 0 | |a Guo-Kai Liu |e author |
245 | 0 | 0 | |a Facile Entry to Pharmaceutically Important 3-Difluoromethyl-quinoxalin-2-ones Enabled by Visible-Light-Driven Difluoromethylation of Quinoxalin-2-ones |
260 | |b MDPI AG, |c 2022-12-01T00:00:00Z. | ||
500 | |a 10.3390/ph15121552 | ||
500 | |a 1424-8247 | ||
520 | |a 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. | ||
546 | |a EN | ||
690 | |a 3-CF<sub>2</sub>H-quinoxaline-2-ones | ||
690 | |a difluoromethylation | ||
690 | |a <i>S</i>-(difluoromethyl)sulfonium salt | ||
690 | |a fluorine-containing pharmaceuticals | ||
690 | |a Medicine | ||
690 | |a R | ||
690 | |a Pharmacy and materia medica | ||
690 | |a RS1-441 | ||
655 | 7 | |a article |2 local | |
786 | 0 | |n Pharmaceuticals, Vol 15, Iss 12, p 1552 (2022) | |
787 | 0 | |n https://www.mdpi.com/1424-8247/15/12/1552 | |
787 | 0 | |n https://doaj.org/toc/1424-8247 | |
856 | 4 | 1 | |u https://doaj.org/article/f4b39e4bd6564fe2b53f6c1407b2e32c |z Connect to this object online. |