2-(2,4-Difluorophenyl)-1,3-bis(1H-1,2,4-triazol-1-yl)propan-2-ol and its pharmaceutically acceptable acid addition salts are disclosed. This particular bis-triazole derivative and its aforesaid salts are useful for treating fungal infections in animals, including humans. Methods for preparing these compounds from known starting materials are provided.
A process for preparing fluconazole, including the steps of (1) acylating 1,3-difluorobenzene (DFB) to obtain 2-chloro-2',4'-difluoroacetophenone (CAP); (2) alkylating 4-amino-4H-1,2,4-triazole (4-AT) with CAP to obtain 2-(1H-1,2,4-triazol-1-yl)-2',4'-difluoroacetophenone (TAAP) salt; (3) deaminating TAAP salt to obtain TAAP; and (4) reacting TAAP with 1,2,4-triazole to obtain fluconazole.
The invention provides a regiospecific process for the preparation of 1,3-bis(1,2,4-triazol-1-yl)-propan-2-ol derivatives comprising reacting an oxirane acid salt or an oxirane, under acidic conditions, with 4H-4-amino-1,2,4-triazole. The process is particularly useful for preparing fluconazole which is useful in the treatment of fungal infections in animals and humans.
1-Triazolyl-2-aryl-3-(5-trifluoromethylimidazol-1-yl)propan-2-ol derivatives useful in the treatment of fungal infections in humans, animals and plants, and their preparation.
Compounds of the formula ##STR1## wherein X is an amine function and R is substituted phenyl and their pharmaceutically acceptable salts are useful antifungal agents in animals, including man.
