| abstract |
Preparation of 2-(2,4-difluorophenyl)-1,3-bis-(1H-1,2,4-triazol-1-yl)-propan-1-ol (fluconazole) of formula (I) and its salts involves reacting a 2-(2,4-difluorophenyl)-1-hydrazino-propan-2-ol derivative of formula (IV) or its salt with s-triazine in an organic solvent under acidic conditions at -60 deg C to reflux temperature. Ar = 2,4-difluorophenyl; R = H, benzyl, triphenylmethyl or COOR1; R1 = alkyl or aryl, preferably tert. butyl or ethyl; Z = triazolyl or NHNHR. Compounds (IV) and their salts are new. Also new are intermediate halo compounds of formula (VIII). |