| 4-甲基-2-正丙基-6-甲氧羰基苯并咪唑的合成 |
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| 引用本文： | 章军,周智明,周磊,余伟发,薛为哲. 4-甲基-2-正丙基-6-甲氧羰基苯并咪唑的合成[J]. 中国新药杂志, 2006, 15(11): 889-891 |
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| 作者姓名： | 章军 周智明 周磊 余伟发 薛为哲 |
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| 作者单位： | 1. 北京理工大学,理学院化学系,北京,100081
2. 北京理工大学,新医药研究开发中心,北京,100081 |
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| 摘 要： | 目的：合成抗高血压药替米沙坦的重要中间体4-甲基-2-正丙基-6-甲氧羰基苯并咪唑.方法：以3-甲基-4-氨基苯甲酸甲酯为原料,经酰化、硝化、还原、环合4步反应制得目标化合物.结果：文献报道的相应各步反应条件得以优化,产率由39.6%提高到62.54%.结论：本方法简化了操作步骤,优化了反应条件,降低了成本,提高了收率.
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| 关 键 词： | 4-甲基-2-正丙基-6-甲氧羰基苯并咪唑 药物合成 替米沙坦 |
| 文章编号： | 1003-3734（2006）11-0889-03 |
| 收稿时间： | 2006-02-10 |
| 修稿时间： | 2006-02-10 |
Synthesis of 2-n-propyl-4-methyl-6- ( methoxycarbonyl ) -benzimidazole |
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| ZHANG Jun,ZHOU Zhi-ming,ZHOU Lei,YU Wei-fa,XUE Wei-zhe. Synthesis of 2-n-propyl-4-methyl-6- ( methoxycarbonyl ) -benzimidazole[J]. Chinese Journal of New Drugs, 2006, 15(11): 889-891 |
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| Authors: | ZHANG Jun ZHOU Zhi-ming ZHOU Lei YU Wei-fa XUE Wei-zhe |
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| Abstract: | Objective: To synthesize 2-n-propyl-4-methyl-6-(methoxycarbonyl)-benzimidazole. Methods: Starting from methyl 4-amino-3-methylbenzoate, the target compound was synthesized via ami-dation, nitration, catalytic reduction and cyclization. Results: The total yield was 62. 54% compared to the yield of 39. 8% reported in a literature. Conclusion: This synthetic procedure optimizes reaction conditions with lower cost and higher yield, and is worthy to have a further pilot manufacture. |
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| Keywords: | 2-n-propyl-4-methyl-6-(methoxycarbonyl) -benzimidazole synthesis telmisartan |
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