New Antifungal 1,2,4-Triazoles with Difluoro(heteroaryl)methyl Moiety
スポンサーリンク
概要
- 論文の詳細を見る
New 1,2,4-triazoles (1) having a difluoro(heteroaryl)methyl moiety were designed and synthesized via 1-aryl-2,2-difluoro-2-(heteroaryl)ethanones (2), which were prepared by two routes starting from the reaction of ethyl 2,2-difluoro(heteroaryl)acetate with phenyllithiums (Route A) and from the reaction of chlorodifluoro(heteroaryl)methane with benzaldehydes (Route B). The compounds 1 except for 1g show antifungal activities against yeasts and filamentous fungi in vitro, especially (+)-1f have equal or superior activities compared to those of itraconazole.
- 公益社団法人日本薬学会の論文
- 2000-07-01
著者
-
Kaneko Yasushi
Central Research Labs. Ss Pharmaceutical Co. Ltd.
-
Sakamoto Takao
Graduate School Of Pharmaceutical Sciences Tohoku University
-
Eto Hiromichi
Central Research Labs. Ss Pharmaceutical Co. Ltd.
関連論文
- Synthesis of β- and γ-Carbolines and Their N-Oxides from 2(or 3)-Ethynylindole-3(or 2)-carbaldehydes
- Convenient Indole Synthesis from 2-Iodoanilines and Terminal Alkynes by the Sequential Sonogashira Reaction and the Cyclization Reaction Promoted by Tetrabutylammonium Fluoride (TBAF)
- Synthesis of 2, 3-Disubstituted Indole Using Palladium(II)-Catalyzed Cyclization with Alkenylation Reaction
- A Concise Synthesis of Furostifoline by Tetrabutylammonium Fluoride-Promoted Indole Ring Formation
- New Antifungal 1, 2, 4-Triazoles with Difluoro(substituted sulfonyl)methyl Moiety
- α, α-gem-Difluorination of α-(Alkylthio)acetophenone Derivatives with N-Fluoropyridinium Salts
- New μ-Opioid Receptor Agonists with Phenoxyacetic Acid Moiety
- New μ-Opioid Receptor Agonists with Piperazine Moiety
- New Strong Fibrates with Piperidine Moiety
- The Cyclization Reaction of Ortho-Ethynylbenzalddehyde Derivatives into Isoquinoline Derivatives
- Efficient Synthesis of 3-Substituted Indazoles Using Pd-Catalyzed Intramolecular Amination Reaction of N-Tosylhydrazones
- The New Method for Introduction of an Allyl Group into the Angular Position of 2-(TBS-oxymethyl)-2,3,4,6,7,8-hexahydro-1-benzopyran-5-one and Its Application to Chiral Wieland-Miescher Type Compound Synthesis
- New Antifungal 1,2,4-Triazoles with Difluoro(heteroaryl)methyl Moiety
- Highly Regioselective Palladium-Catalyzed Annulation Reactions of Heteroatom-Substituted Allenes for Synthesis of Condensed Heterocycles