PURPOSE: To produce a new triazole derivative having a remarkably strong antifungal effect and effective for treating the infection of a superficial mycotis or mycotis profundus to an animal or a human.
CONSTITUTION: A compound of formula I (R1 and R2 are both H or one of them is H and the other is a lower alkyl. Or, ethylene is formed in combination of R1 with R2; R3 is an alkyl; R4 is H, a lower alkyl or a halogen; (n) is 1 or 2) or its physiologically permissible salt, e.g. (2R*, 3R*)-2-(2,4- difluorophenyl)-3-[4(methylsulfinyl)phenoxy]-1-(1H-1,2,4,-triazol-1-yl)butan-2-ol. This compound can be synthesized by allowing a Friedel-Crafts reaction between m-difluorobenzene of formula II and an αhalogen-substituted acid halide of formula III to take place, reacting the resultant acyl compound of formula IV with a compound of formula V, converting the obtained ketone compound into an oxirane compound of formula VII and reacting the compound of formula VII satisfying (m)=1 or 2 with 1,2,4-triazole (alkaline metal salt).
TAKAGI JUN
TSUJI NORITOSHI
SAKUMA OSAMU
OOTO HIROYUKI
IWASE YOKO
