FLUCONAZOLE-CONTAINING MEDICINAL AGENT AND METHOD OF SYNTHESIS OF FLUCONAZOLE Russian patent published in 2001 - IPC

FIELD: organic chemistry, chemical technology, pharmacy, pharmaceutical technology. SUBSTANCE: invention relates to method of synthesis of fluconazole that is a medicinal agent eliciting the antifungal effect. For synthesis of fluconazole 2,4-difluoro-2-(1H-1,2,4-triazole-1)-yl-acetophenone, 1,2,4-triazole and trimethylsulfoxonium iodide are mixed in an aqueous alkaline solution, reactive mixture is heated at 43-49 C for 12-23 h followed by addition of methylene chloride. Then organic layer is washed out with water at pH = 8.5-9.5, methylene chloride is removed at 43-49 C, washed out with isopropyl alcohol, cooled and kept for 8-12 h at 6-8 C and the end product is separated. Claimed substance of fluconazole can be used for storage both as pure form and as component of medicinal forms. EFFECT: improved method of synthesis, enhanced stability of fluconazole. 4 cl, 3 tbl, 3 ex