- New antifungal 1,2,4-triazoles with difluoro(substituted sulfonyl)methyl moiety
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New 1,2,4-triazoles (2) having a difluoro(substituted sulfonyl)methyl moiety were designed and synthesized via α,α-difluoro-α-(substituted thio)acetophenones (3). Compounds (2) showed potent antifungal activities against C. albicans, C. krusei, A. flavus
- Eto,Kaneko,Takeda,Tokizawa,Sato,Yoshida,Namiki,Ogawa,Maebashi,Ishida,Matsumoto,Asaoka
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p. 173 - 182
(2007/10/03)
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- Preparation process of difluoroacetophenone derivative
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The invention relates to a process for preparing a difluoroacetophenone derivative (4) by alkylthionating a compound (1) into a compound (2) and reacting this compound with a compound (3). wherein X1is Cl, Br or I, X2and X3/sup
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- α, α-gem-difluorination of α-(alkylthio)acetophenone derivatives with N-Fluoropyridinium salts
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The α, α-gem-difluorination of 2',4'-difluoro- α(methylthio)acetophenone (1a) with N-fluoropyridinium salts gave 2',4',α-tetrafluoro-α-(methylthio)acetophenone (3a). This reaction was accelerated by the addition of zinc chloride, zinc bromide or anhydrous iron(III) chloride, and higher yields than the reaction without additives were obtained. The gem- difluorination reaction using FP-T300 in the presence of zinc bromide was applicable to other α-(alkylthio)acetophenone derivatives (1).
- Takeda, Sunao,Kaneko, Yasushi,Eto, Hiromichi,Tokizawa, Minoru,Sato, Susumu,Yoshida, Kouiti,Namiki, Setsuo,Ogawa, Masaki
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p. 1097 - 1100
(2007/10/03)
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- Triazole derivative and pharmaceutical comprising the same as an effective ingredient
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Described is a triazole derivative represented by the formula (1) or salt thereof, preparation process thereof, preparation intermediates represented by the formulas (2) and (3), and a pharmaceutical comprising the compound represented by the formula (1)
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