METHOD OF SYNTHESIS OF FLUCONAZOLE Russian patent published in 2001 - IPC

FIELD: organic chemistry, chemical technology, pharmaceutical technology. SUBSTANCE: invention relates to method of synthesis of drug fluconazole showing antifungal effect. Method of synthesis of fluconazole involves mixing 2,4-difluoro-1H-1,2,4-triazole-1-yl-acetophenone, 1,2,4-triazole and trimethylsulfoxonium iodide in alkaline aqueous solution and mixture is kept at 4-25 C. Then reaction mixture is heated at 45-50 C for 6-28 h, methylene chloride is added, organic layer is washed out with water at pH = 8.5-9.5, methylene chloride is removed at 45-50 C, washed out with toluene followed by its removal at 45-50 C, kept for 0.5-2 h, washed out again with toluene at 25-30 C and dried at 60-65 C for 8-12 h. EFFECT: increased stability and purity of fluconazole. 4 tbl