Process for preparing triazole antimycotic compounds

Details Process for preparing triazole antimycotic compounds Process for preparing triazole antimycotic compounds

C - Chemistry, Metallurgy

07

D

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

Patent

CA 2313001

Process for the preparation of a compound of formula (VII) wherein R1 is Cl, F or CF3; R2 is H, Cl, F or CF3; and R3 is C1-4 alkyl; characterized in that an olefin of formula (II) is epoxidized to give an oxirane of formula (III) which treated with alkyl-magnesium halide gives a triol of formula (IV) which is turned into an epoxide of formula (V), then treated with 1,2,4-triazole. The compounds (VII) are useful for preparing azole derivatives active as antifungal agent.

L'invention porte sur un procédé de préparation d'un composés de la formule (VII) dans laquelle R¿1? représente Cl, F ou CF¿3?; R¿2? représente H, Cl ou CF¿3?; et R¿3? représente alkyle C¿1-4?. Ce procédé se caractérise en ce qu'une oléfine de la formule (II) est époxidée pour donner un oxirane de la formule (III) qui, traité avec un halogénure d'alkyle-magnésium, donne un triol de la formule (IV) qui est à son tour transformé en un époxide de la formule (V), et traité ensuite avec 1,2,4-triazole. Les composés (VII) sont utilisés dans la préparation de dérivés d'azole agissant comme agents antifongiques.

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