cas 1978-06-9, 2,3-BIS(TRIFLUOROMETHYL)NITROBENZENE

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Structure-activity relationships of antitubercular salicylanilides consistent with disruption of the proton gradient via proton shuttling
A series of salicylanilides was synthesized based on a high-throughput screening hit against Mycobacterium tuberculosis. A free phenolic hydroxyl on the salicylic acid moeity is required for activity, and the structure-activity relationship of the aniline ring is largely driven by the presence of electron withdrawing groups. We synthesized 94 analogs exploring substitutions of both rings and the linker region in this series and we have identified multiple compounds with low micromolar potency. Unfortunately, cytotoxicity in a murine macrophage cell line trends with antimicrobial activity, suggesting a similar mechanism of action. We propose that salicylanilides function as proton shuttles that kill cells by destroying the cellular proton gradient, limiting their utility as potential therapeutics.
Lee, Ill-Young,Gruber, Todd D.,Samuels, Amanda,Yun, Minhan,Nam, Bora,Kang, Minseo,Crowley, Kathryn,Winterroth, Benjamin,Boshoff, Helena I.,Barry III, Clifton E.
p. 114 - 126
(2013/02/22)

THE TRIFLUOROMETHYLATION OF CHLOROAROMATICS USING THE COPPER-CF2Br2-DIALKYLAMIDE REACTION SYSTEM
The in situ generation of CuCF3 from the reaction of copper, dibromodifluoromethane and either N,N-dimethylformamide or N,N-dimethylacetamide (Burton's reagent) has been used for the direct substitution of chlorine by CF3 in a number of aromatic substrates.Particular attention has been paid to the effects of ring substituents on the efficiency of reaction.
Clark, James H.,Denness, James E.,McClinton, Martin A.,Wynd, Andrew J.
p. 411 - 426
(2007/10/02)