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苯磺酸氨氯地平的合成研究
Synthesis of amlodipine besylate
【摘要】 目的研究钙离子拮抗剂苯磺酸氨氯地平的合成。方法自行设计苯磺酸氨氯地平的合成路线,以氨基乙醇和邻苯二甲酸酐为起始原料,经缩合、Hantzsch合成、还原、成盐反应得到目标化合物。结果经6步反应制得目标化合物,总收率为38.4%。目标化合物结构经IR1、H-NMR、MS等确证。结论设计了一条未见文献报道的新的合成路线,与文献方法相比,该合成工艺具有原料易得、反应条件温和、操作简便、收率较高等优点。
【Abstract】 Aim To study the synthetic process of amlodipine besylate,an calcium-channel antagonist.Methods Amlodipine besylate were designed and synthesized from ethanolamine and phthalic anhydride via condensation,Hantzsch synthesis,reduction,and salt formation.Results The target compound was obtained via six steps and identified by IR,()~1H-NMR and MS.The total yield was 38.4%.Conclusion In comparison with the method reported,this method has several advantages of cheap reagents,facile reaction conditions,convenient operation and high yield.
【Key words】 medicinal chemistry; drug preparation; chemical synthesis; amlodipine besylate; calcium antagonist;
- 【文献出处】 中国药物化学杂志 ,Chinese Journal of Medicinal Chemistry , 编辑部邮箱 ,2006年03期
- 【分类号】R914.5
- 【被引频次】6
- 【下载频次】1493