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2-正丁基-5-甲酰基咪唑的合成
引用本文:严青松,陈玉彬. 2-正丁基-5-甲酰基咪唑的合成[J]. 中国药物化学杂志, 2008, 18(2): 123-125
作者姓名:严青松  陈玉彬
作者单位:沈阳药科大学制药工程学院,辽宁,沈阳,110016
摘    要:目的合成抗高血压药伊普沙坦的关键中间体2-正丁基-5-甲酰基咪唑。方法乙二胺与戊腈在硫粉的作用下环合得到2-正丁基咪唑啉(2),经脱氢、碘化、还原、羟甲基化、氧化、催化氢解得到目标化合物2-正丁基-5-甲酰基咪唑(1)。结果与结论目标化合物的结构经MS、^1H-NMR谱确证,优化后的合成路线,所用试剂易得、操作简单、反应条件温和,总收率为10.8%。

关 键 词:2-正丁基-5-甲酰基咪唑  合成  抗高血压  伊普沙坦
文章编号:1005-0108(2008)02-0123-03
收稿时间:2007-08-27
修稿时间:2007-08-27

Synthesis of 2-butyl-5-formylimidazole
YAN Qing-song,CHEN Yu-bin. Synthesis of 2-butyl-5-formylimidazole[J]. Chinese Journal of Medicinal Chemistry, 2008, 18(2): 123-125
Authors:YAN Qing-song  CHEN Yu-bin
Affiliation:School of Pharmaceutical Engineering Shenyang Pharmaceutical University, Shenyang 110016, China)
Abstract:Aim To synthesize a key intermediate of eprosartan, 2-butyl-5-formylimidazole(1). Methods With ethylenediamine and valeronitrile as raw materials, 2-butyl-imidazoline (2) was synthesized in the presence of sulfur, after dehydrogenation, iodination, reduction, hydroxymethylation, oxidation, hydrogenolysis to give 2-butyl-5-formylimidazole. Results and conclusion Aimed compound was synthesized and identified by MS and 1H-NMR. The starting materials in the synthetic route are easily available and this procedure has advantage of convenient operations and mild conditions. The total yield is 10.8%.
Keywords:2-butyl-5-formylimidazole  synthesis  antihypertension  eprosartan
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