| 沙美特罗的一条新合成路线 |
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| 引用本文： | 周玓,刘军涛,鲁毅翔,贾娴,黎星术.沙美特罗的一条新合成路线[J].中国药物化学杂志,2009,19(2). |
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| 作者姓名： | 周玓 刘军涛 鲁毅翔 贾娴 黎星术 |
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| 作者单位： | （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） |
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| 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 总收率18%。结论 本路线合成成本低廉，适用于大量制备。
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| 关 键 词： | 沙美特罗 β2-肾上腺能受体激动剂 合成 |
| 收稿时间： | 2008-9-22 |
| 修稿时间： | 2009-1-20 |
New synthetic route to salmeterol |
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| ZHOU Di,LIU Jun-tao,LU Yi-xiang,JIA Xian,LI Xing-shu.New synthetic route to salmeterol[J].Chinese Journal of Medicinal Chemistry,2009,19(2). |
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| Authors: | ZHOU Di LIU Jun-tao LU Yi-xiang JIA Xian LI Xing-shu |
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| Institution: | (1.School of Pharmaceutical Engineering, Shenyang Pharmaceutical University, Shenyang, 110016, China; 2.School of Pharmaceutical Science, Sun Yat-sen University, Guangzhou 510080, China) |
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| Abstract: | 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. Result The overall yield was 18%. Conclusions The new synthetic route is suitable for large scale preparation with low cost. |
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| Keywords: | salmeterol β2-adrenegic agonist synthesis |
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