The direct C3-functionalization of quinoxalin-2(1H)-ones via C–H bond activation has recently attracted considerable attention, due to their diverse biological activities and chemical properties.
Aryl trifluoromethyl ketone is a very important intermediate in the organic synthesis. Much attention has been attracted from researchers, due to its potential bioactivity. In this paper, the recent progress in the synthesis of aryl trifluoromethyl ketone is reviewed, including the oxidant of α-trifluoromethyl alcohols, trifluoromethylation of carboxylic acid derivatives, trifluoroacetylation of organometallic reagents, electron-rich aromatics, aryl halides and aryl diazonium salts, and the reaction mechanisms are also discussed.
Direct trifluoroacetylation of indoles with ethyl trifluoropyruvate as a trifluoroacetylating reagent has been developed. This novel protocol provides an attractive route for the preparation of 3-trifluoroacetylindole derivatives, due to its operational simplicity and practicability as well as mild reaction conditions.
A novel copper(I)-mediated trifluoroacetylation of anilines with ethyl trifluoropyruvate as a
trifluoroacetylating reagent has been developed. Although this protocol could provide good yields in
most cases, the reaction exhibited the obvious electronic and steric effects of substituents. The trace
amount of products was only obtained for the substrates with ortho-substituted or electron-deficient
groups.
An approach has been developed for the copper-catalyzed acetylation of phenols and anilines with potassium thioacetate as an acetylating reagent. Although only electron-rich phenols and anilines are compatible with this protocol, the reaction can provide moderate to high yields under mild conditions. Compared with other acetylating reagents, the current reagent has certain advantages, such as its low cost, easy availability, stability, insensitivity to water or air, and ease of storage.
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