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罗沙替丁衍生物的合成

Synthesis of Roxatidine Derivatives

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【作者】 张辉张倩云林莉程卯生

【Author】 ZHANG Hui1,ZHANG Qian-yun2,LIN Li1,CHENG Mao-sheng3(1.Department of Chemistry,Shenyang Medical College,Shenyang 110034,China;2.College of Commonality Health,China Medical University,Shenyang 110001,China;3.School of Pharmaceutical Engineering,Shenyang Pharmaceutical University,Shenyang 110016,China)

【机构】 沈阳医学院化学教研室中国医科大学公共卫生学院沈阳药科大学制药工程学院 辽宁沈阳110034辽宁沈阳110001辽宁沈阳110034辽宁沈阳110016

【摘要】 以间羟基苯甲醛为原料,经3步反应合成了N-{3-[3-(1-甲基哌啶)苯氧基]丙基}氯乙酰胺(3);3与乙酸钾反应得到H2-受体拮抗剂罗沙替丁乙酸酯盐酸盐;3与伯胺反应合成了4个罗沙替丁的衍生物,再与草酸成盐得对应的草酸盐,其结构经1H NMR,IR和MS表征。

【Abstract】 N-{3-[3-(1-methylpiperidine)phenoxy]propyl}chloroacetamide(3) was synthesized by a three-step reaction from m-hydroxyl-benzaldehyde.Salt of roxatidine acetic ester with hydrochloric acid was prepared by the reaction of 3 with AcOK.Four roxatidine derivatives were synthesized by the reaction of 3 with primary amine and then with oxalic acid to obtain thier salts.The structures were confirmed by 1H NMR,IR and MS.

  • 【文献出处】 合成化学 ,Chinese Journal of Synthetic Chemistry , 编辑部邮箱 ,2008年03期
  • 【分类号】TQ463.53
  • 【被引频次】2
  • 【下载频次】235
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