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Showing 1 to 5 of 5 for “"trifluoromethyl ketones"”.
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Trifluoromethyl ketones: Potential insecticides towards Anopheles gambiae
… In vitro assay studies have shown that trifluoromethyl ketones (TFK's) are potent inhibitors of An. gambiae AChE (AgAChE), that inhibit the enzyme by making a covalent adduct with the catalytic serine of the enzyme. However research in the Carlier group has shown that trifluoromethyl …
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Synthesis of Delta(3)-Imidazolines as Latent Forms of Peptidyl Trifluoromethyl Ketones
Many trifluoromethyl-substituted imidazolines were efficiently synthesized directly into larger peptides, by use of carbamate-protected amino acid fluorides as the initiator of the dipolar cycloaddition. The imidazolines then functioned as a protecting group for the trifluoromethyl ketones during …
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Entwicklung von Carben-katalysierten asymmetrischen intermolekularen Stetter-Reaktionen und direkt gekreuzter intermolekularer Benzoin-Reaktionen
… Stetter reaction. The resulting 1,4-diketones were obtained in moderate to excellent yields (49-98%) and good enantioselectivities (56-78% ee). For several Stetter products the enantiomeric excess could be enhanced by a single recrystallization up to 99% ee. Examination of the reaction …
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Development of decarboxylative strategies towards the synthesis of fluorinated pharmacons
Fluoro(oxo) functional groups, such as trifluoromethyl ketones, difluoromethyl ketones, and trifluoroethanols, have emerged as desirable motifs in medicinal chemistry for the fine tuning of pharmacokinetic properties. Over the past few decades, fluoro(oxo) diversity has been accessed through …
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Fluoromethyl ketone prodrugs: Potential new insecticides towards Anopheles gambiae
… studies demonstrate that tri- and difluoromethyl ketones can potentially inhibit An. gambiae AChE (AgAChE). These compounds inhibit the enzyme by making a covalent adduct with the catalytic serine of AChE. Trifluoromethyl ketones however are poor inhibitors of the G119S resistant mutant of AgAChE. …