硫酸头孢喹肟的合成

Synthesis of cefquinome sulfate

研究第四代头孢类抗生素硫酸头孢喹肟的合成工艺。以7-氨基头孢烷酸(7-ACA)为原料,在三甲基碘硅烷的作用下与5,6,7,8-四氢喹啉缩合,得到中间体7-氨基头孢喹肟(7-ACQ),7-ACQ直接与AE活性酯反应,得到头孢喹肟硫酸盐,总收率51.9%。用元素分析,IR与1H NMR对其结构进行了鉴定。该合成路线适合工业化生产。

The synthetic route and improved process for the preparation of cefquinome sulfate were studied. In the presence of trimethyliodosiliane, 7-ACA, which underwent 3-substitution by 5,6,7,8-tetrahydroquinohne and then reacted with AEME, cefquinome sulfate was obtained in 51.9% overall yield. The structure of target substance was determined by elemental analysis, IR and ^1H NMR. This synthetic route is suitable for industrial manufacture.