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。 Objective To study the new synthetic route of metoprolol. Methods Starting from p-hydroxybenzaldehyde, Darzen condensation with ethyl chloroacetate occurred after benzyl protection and rearranged to give 4-benzyloxyphenylacetaldehyde, which was further reacted with sodium bisulfite Addition, and finally by potassium borohydride reduction, methyl etherification, deprotection, etherification, amination reaction of the target compound. Results and Conclusions The structures of target compounds were confirmed by IR, MS, 1H-NMR and 13C-NMR. The synthesis route is easy to operate and requires fewer intermediates to be purified for industrial production.