琥珀酸美托洛尔的合成工艺改进

目的 优化琥珀酸美托洛尔的合成路线.方法 以4-(2-甲氧基乙基)苯酚和环氧氯丙烷为原料在相转移催化剂四丁基溴化铵催化下,先得到1-(2,3-环氧丙氧基)-4-(2-甲氧基乙基)-苯;再与异丙胺在催化剂AlCl3的作用下反应,得到美托洛尔;最后将美托洛尔与琥珀酸的饱和乙醇溶液反应即得琥珀酸美托洛尔.结果 目标化合物琥珀酸美托洛尔的结构经核磁共振氢谱(1 H-NMR)和电喷雾质谱法(ESI-MS)确证,高效液相色谱法测定纯度为99.01%,总收率为51.8%.结论 本实验工艺简单,反应时间短,收率较高,产品纯度好,而且在较大程度上降低了环境污染,绿色环保.

Improved technology for synthesis of metoprolol succinate

Objective To improve the synthesis process of metoprolol succinate.Methods p-(2-Methoxyethyl) phenol and epichlorohydrin were taken as starting reagents. Tetrabutylammonium bromide was used to catalyze their reaction to get 1-(2,3-epoxypropoxy)-4-(2-methoxyethyl) benzene.And then AlCl₃ was used to catalyze the reaction of 1-(2,3-epoxypropoxy)-4-(2-methoxyethyl) benzene and isopropyl amine to obtain metoprolol.Finally,metoprolol was treated with succinic acid to get metoprolol succinate.Results The structure of metoprolol succinate was corroborated by ¹H-NMR and ESI-MS.The purity was 99.01%,while the total yield was 51.8%.Conclusion This method was simple,moderate and environmentally- friendly.The product purity and yield were all high.It was suitable for industrialization of green production.