| 溴莫普林的合成 |
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| 引用本文： | 金熔 王尔华. 溴莫普林的合成[J]. 中国药科大学学报, 2000, 31(1): 1-2 |
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| 作者姓名： | 金熔 王尔华 |
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| 作者单位： | 中国药科大学医药化工研究所!南京210009 |
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| 摘 要： | 以 4 溴 3,5 二羟基苯甲酸为起始原料 ,经甲基化 酯化、肼化、氧化得 4 溴 3,5 二甲氧基苯甲醛 ,与丙烯腈缩合 ,再与硝胍环合得标题化合物 ,总收率为 2 9%。
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| 关 键 词： | 溴莫普林 甲氧苄氨嘧啶 合成 二羟基苯甲酸 |
| 修稿时间： | 1999-09-22 |
Synthesisof Brodimoprim |
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| JIN Rong,WANG Er Hu,YANG You Tian Medicinal and Chemical Institute,China Pharmaceutical University,Nanjing. Synthesisof Brodimoprim[J]. Journal of China Pharmaceutical University, 2000, 31(1): 1-2 |
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| Authors: | JIN Rong WANG Er Hu YANG You Tian Medicinal Chemical Institute China Pharmaceutical University Nanjing |
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| Affiliation: | JIN Rong,WANG Er Hua,YANG You Tian Medicinal and Chemical Institute,China Pharmaceutical University,Nanjing 210009 |
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| Abstract: | An improved process for the preparation of brodimoprim(1) was described. Compound 1 was synthesized from 4 bromo 3,5 dimethoxy benzoic aldehyde(5) by condensation with acrylonitrile and cyclization with guanidine nitrate. The compound 5 was prepared form 4 bromo 3,5 dihydroxy benzoic acid through methylation esterification, hydrazination and oxidation. The overall yield was 29%. |
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| Keywords: | Dihydrofolate reductase inhibitor Brodimoprim Trimethoprime Synthesis |
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