Journal
ADVANCED SYNTHESIS & CATALYSIS
Volume 360, Issue 20, Pages 3969-3977Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201800863
Keywords
C-H Trifluoromethylation; Transition-Metal-Free; Sodium trifluoromethanesulfinate; Quinoxalin-2(1H)-ones
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Funding
- National Natural Science Foundation of China [21776056]
- Natural Science Foundation of Hebei Province [B2018202253, B2016202393, B2015202284]
- Program for the Top Young Innovative Talents of Hebei Province [BJ2017010]
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Disclosed herein is a direct C-H trifluoromethylation of quinoxalin-2(1H)-ones with sodium trifluoromethanesulfinate. This protocol affords a series of 3-trifluoromethylquinoxalin-2(1H)-one derivatives in moderate to excellent yields under transition-metal-free conditions. The present methodology features utilization of the inexpensive trifluoromethyl source without transition-metal-catalysts, mild reaction conditions and high functional group tolerance, which promises a convenient and efficient access to pharmaceutically interesting quinoxalinones.
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