格列美脲是新一代磺酰脲类降糖药 ,具有高效、长效、副作用小等优点 .以乙酰乙酸乙酯为原料 ,先制得关键中间体 3 乙基 4 甲基 3 吡咯啉 2 酮 (Ⅳ ) ,然后与 β 苯乙基异氰酸酯 (Ⅴ )缩合 ,再经磺化、氨解等反应制得格列美脲 ,总收率为 13.39% .该合成路线具有原料易得、反应条件温和、后处理方便、三废少等优点 ,适合工业规模制备格列美脲 Glimepiride is a new generation of sulfonylurea hypoglycemic agents, with the advantages of high efficiency, long-acting, small side effects, etc. With ethyl acetoacetate as the raw material, the key intermediate 3 ethyl 4 methyl 3 pyrroline 2 ketone (Ⅳ), and then with p-phenylethyl isocyanate (Ⅴ) condensation, and then by sulfonation, ammonolysis reaction of glimepiride, the total yield was 13.39%. The synthetic route with raw materials readily available, mild reaction conditions , Post-processing convenience, less waste, etc., suitable for industrial scale preparation glimepiride