Process for preparing triazole compounds

Details Process for preparing triazole compounds Process for preparing triazole compounds

C - Chemistry, Metallurgy

07

D

C07D 249/08 (2006.01) C07D 521/00 (2006.01)

Patent

CA 2312785

Process for the preparation of a compound of formula (VIII) wherein R1 is Cl, F or CF3; R2 is H, Cl, F or CF3; and R3 is C1-4 alkyl; characterized in that a triol of formula II is treated with a ketone or an aldehyde to give a dioxolane of formula III which by treatment with an aryl-methyl halide gives the compound of formula IV which is hydrolyzed to give a compound of formula V which is functionalized on the primary hydroxy group by a leaving group Lg and treated with a salt of 1,2,4-triazole. The compounds (VIII) is useful for preparing azole derivatives active as antifungal agent.

L'invention porte sur un procédé de préparation d'un composé de la formule (VIII) dans laquelle R¿1? représente Cl, F ou CF¿3?; R¿2? représente H, Cl, F ou CF¿3?; et R¿3? représente alkyle C¿1-4?. Ce procédé se caractérise en ce qu'un triol de la formule II est traité avec une cétone ou un aldéhyde pour donner un dioxolane de la formule III qui, traité avec un halogénure aryle-méthyle donne le composé de la formule IV qui est hydrolysé pour donner un composé de la formule V fonctionnalisé sur le groupe hydroxy primaire par un groupe labile Lg et traité avec un sel de 1,2,4-triazole. Les composés (VIII) sont utiles dans la préparation de dérivés d'azole agissant comme agents antifongiques.

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