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- W2036476360 abstract "In the search for new potent antiparasitical fluoroquinolones, a QSAR analysis by molecular connectivity led to the design of R5 (Me or Et)/R8 (MeO, Me or Et)-substituted analogs of the most powerful antibacterial or antiparasitical fluoroquinolones known so far. Unfortunately, the synthetic schemes that were elaborated in literature for 3- and 3,6-di-substituted 2,4,5-trifluorobenzoic acids, the key precursors of the target R5/R8-substituted 6-fluoroquinolones, led in our hands to poor yields and/or to inextricable mixtures of derivatives. This led us to reinvestigate the key alkylation steps of the 2,4,5-trifluorophenyl-oxazoline synthons and the subsequent deprotection of their oxazoline into acid with the aim of optimising the syntheses of 3- and 3,6-di-substituted 2,4,5-trifluorobenzoic acids, which constitute the entries to our target derivatives." @default.
- W2036476360 created "2016-06-24" @default.
- W2036476360 creator A5007253219 @default.
- W2036476360 creator A5091904705 @default.
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- W2036476360 date "2005-08-01" @default.
- W2036476360 modified "2023-09-25" @default.
- W2036476360 title "Synthesis of mono- and di-substituted 2,4,5-trifluorobenzoic acid synthons, key precursors for biologically active 6-fluoroquinolones" @default.
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- W2036476360 doi "https://doi.org/10.1016/j.tet.2005.06.078" @default.
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