沙美特罗的一条新合成路线

New synthetic route to salmeterol

目的研究开发平喘药沙美特罗的新合成路线。方法以对羟基苯甲醛为起始原料经过4步反应得到伯胺5;以苯基丁醇为起始原料,经过3步反应得到脂肪醛8;将5与8经对接、氢化,再经酸性水解去掉保护基得到目标化合物。结果与结论该路线合成成本低廉,总收率18%,适用于大量制备。

Aim To develop a new synthetic route to salmeterol. Methods Compound 5 was synthesized via four steps taking p-hydroxy benzaldehyde as starting material and compound 8 was obtained through three steps starting from phenylbutanol. Then compound 5 reacted with 8 through coupling and hydrogenation reaction, followed by deprotection to afford the target compound. Results The overall yield was 18%. Conclusion The new synthetic route is suitable for large scale preparation with low cost.