拉夫替丁的合成 |
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引用本文: | 陶锋,吕春绪. 拉夫替丁的合成[J]. 中国医药工业杂志, 2004, 35(7): 393-395 |
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作者姓名: | 陶锋 吕春绪 |
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作者单位: | 1. 江苏亚邦集团公司医药研究所,江苏,常州,213163 2. 南京理工大学,江苏,南京,210009 |
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摘 要: | 2-氨基-4-甲基吡啶经溴代、氧化、还原、再氧化成醛、与乙二醇成缩醛后醚化得2-[4-(四氢吡喃-2-基氧基)-(2Z)-丁烯基氧基]-4-(1,3-二氧戊环-2-基)吡啶,再将脱THP保护基、Gabriel反应、肼解一锅合成,然后经酰胺化和缩醛水解、与哌啶缩合等反应制得H2受体拮抗剂拉夫替丁,总收率6.8%.
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关 键 词: | 拉夫替丁 H2受体拮抗剂 抗溃疡药物:合成 |
文章编号: | 1001-8255(2004)07-0393-03 |
Synthesis of Lafutidine |
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Abstract: | Lafutidine, a histamine H2-receptor antagonist, was synthesized from 2-amino-4-methylpyridine bybromination, oxidation, reduction, oxidation, etherification to give 2-[4-(tetrapyran-2-yloxyl)-(2Z)-buten-oxy]-4-(1,3-dioxolan-2-yl)pyridine which subjected to hydrolysis, chlorination, Gabriel reaction, hydrazinolysis in one pot followed byamidation, hydrolysis and then condensation with piperidine in an overall yield of 6.8%. |
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Keywords: | lafutidine histamine H2-receptor antagonist anti-ulcer synthesis |
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