第 43 卷第 2 期 | | Vol. 43 No. 2 | 2013 年 4 月 | Apr 2013 |
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所属栏目:医药及中间体
盐酸替罗非班的合成研究 |
刘 超,陆旭芳,耿元硕,李志裕*
(中国药科大学 药物化学教研室,江苏 南京 210009) |
摘 要:以4-(4-哌啶基)-1-氯丁烷、L-酪氨酸等为原料经过7步反应得到盐酸替罗非班。此合成路线操作简易,总收率达21.6%,中间体及最终产物结构均经过MS和1H NMR确证。 |
关键词:血小板GP IIb/IIIa 受体拮抗剂;盐酸替罗非班;合成 |
中图分类号:R737.902 文献标识码:A 文章编号:1009-9212(2013)02-0042-04 |
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Synthesis of Tirofiban Hydrochloride |
LIU Chao,LU Xu-fang,GENG Yuan-shuo,LI Zhi-yu*
(Department of Medicinal Chemistry,China Pharmaceutical University,Nanjing 210009,China) |
Abstract:Tirofiban hydrochloride is a reversible non-peptide platelet GP IIb/IIIa receptor antagonist,for the treatment of acute coronary syndrome. This paper reported the synthesis of Tirofiban hydrochloride from 4-(4-piperidinyl)-1-chlorobutane and L-tyrosine via 7 steps of chemical reactions. This new synthesis route with low-toxicity and simple operation has a high yield which is up to 21.6%. The structures of the intermediates and the final product were certified by MS and 1H NMR. |
Key words:platelet GP IIb/IIIa receptor antagonist;Tirofiban hydrochloride;synthesis |
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作者简介:刘 超(1987-),男,内蒙古呼和浩特人,硕士研究生,主要从事药物活性分子的设计与合成。(E-mail:chaosliu21@163.com)
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联 系 人:李志裕,教授,硕士研究生导师。(E-mail:zhiyuli@cpu.edu.cn)
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收稿日期:2013-04-23
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