美托洛尔的合成新工艺研究

目的 研究美托洛尔的新合成路线。方法 以对羟基苯甲醛为起始原料，经苄基保护后与氯乙酸乙酯发生Darzen缩合、重排反应得中间体4-苄氧基苯乙醛，该中间体再与亚硫酸氢钠进行加成，最后经硼氢化钾还原、甲醚化、脱保护、醚化、胺化反应得目标化合物。结果与结论 目标化合物的结构经 IR、MS、¹H-NMR、¹³C-NMR谱确证。该合成路线操作简便，需要提纯的中间体较少，适合工业化生产。

A novel synthetic technology of metoprolol

Aim To synthesize a novel concise synthetic route for metoprolol. Methods Starting from 4-hydroxybenzaldehyde, 4-benzyloxyphenylacetaldehyde was obtained via benzyl-protection, Darzen condensation and rearrangement reaction. The metoprolol was synthesized by using addition reaction of sodium bisulfite and 4-benzyloxyphenylacetaldehyde, reduction by potassium borohydride, methylation, deprotection, etherification, and amination. Results and conclusion The structure of target compound was confirmed by IR, MS, ¹ H-NMR and ¹³C-NMR. The method is convenient operation without complicate purification and suitable for industrialized production.