沙美特罗的一条新合成路线  

New synthetic route to salmeterol

作　　者：周玓[1] 刘军涛[2] 鲁毅翔[1] 贾娴[1] 黎星术[2] 

机构地区：[1]沈阳药科大学制药工程学院,辽宁沈阳110016 [2]中山大学药学院,广东广州510080

出　　处：《中国药物化学杂志》2009年第2期123-125,139,共4页Chinese Journal of Medicinal Chemistry

基　　金：国家自然科学基金项目(20472116);广州市科技计划攻关项目(4205009);辽宁省博士科研启动基金项目(1050155)

摘　　要：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.

关 键 词：沙美特罗 β2-肾上腺能受体激动剂 合成 

分 类 号：R914[医药卫生—药物化学]