| 长效H2受体拮抗剂-拉呋替丁的合成 |
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| 引用本文： | 朱仁发,王效山,俞汉青.长效H2受体拮抗剂-拉呋替丁的合成[J].合肥工业大学学报(自然科学版),2005,28(10). |
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| 作者姓名： | 朱仁发 王效山 俞汉青 |
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| 作者单位： | 1. 中国科学技术大学,化学系,安徽,合肥,230026
2. 安徽中医学院,药学院,安徽,合肥,230031 |
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| 摘 要： | 以2-溴-4-(哌啶基甲基)吡啶为原料,与2-丁烯-1,4-二醇醚化,经氯化、G abrie l反应、肼解,然后再与2-呋喃甲硫基-S-氧代乙酸对硝基苯酚酯进行胺解反应,制得第二代长效H2受体拮抗剂拉呋替丁,总收率为29.89%以2-溴-4-(哌啶基甲基)吡啶计]。
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| 关 键 词： | 拉呋替丁 H2受体拮抗剂 2-溴-4-(哌啶基甲基)吡啶 合成 抗溃疡药物 |
Synthesis of the novel histamine 2 H2-receptor antagonist-lafutidine |
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| ZHU Ren-fa,WANG Xiao-shan,YU Han-qing.Synthesis of the novel histamine 2 H2-receptor antagonist-lafutidine[J].Journal of Hefei University of Technology(Natural Science),2005,28(10). |
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| Authors: | ZHU Ren-fa WANG Xiao-shan YU Han-qing |
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| Institution: | ZHU Ren-fa~1,WANG Xiao-shan~2,YU Han-qing~1 |
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| Abstract: | The new histamine H_2-receptor antagonist,lafutidine,was synthesized from 2-bromo-4-(methylpiperidyl)pyridine by etherification with 2-butene-1,4-diol,chlorination,Gabriel reaction,and hydrazinolysis which was followed by amidation reaction with 2-(furfurylsulfinyl)acetic acid p-nitrophenyl ester,and an overall yield of 29.89% was achieved. |
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| Keywords: | lafutidine histamine H_2-receptor antagonist 2-bromo-4-(methylpiperidyl)pyridine synthesis antiulcer |
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