| 呋布西林钠的合成工艺改进 |
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| 引用本文： | 马玉卓,刘鹰翔,周玉平,梅文杰,佘志刚. 呋布西林钠的合成工艺改进[J]. 中国药物化学杂志, 2006, 16(1): 51-53 |
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| 作者姓名： | 马玉卓 刘鹰翔 周玉平 梅文杰 佘志刚 |
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| 作者单位： | 1. 广东药学院,药物化学系,广东,广州,510006
2. 中山大学,化学与化学工程学院,广东,广州,510275 |
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| 摘 要： | 以呋喃甲醛为起始原料,经肟化、贝克曼重排、异氰脲酸化、氨基化、缩合和成盐6步反应,合成了酰脲类青霉素抗生素呋布西林钠。该工艺路线使用甲酸钠代替异辛酸钠,减少了关键中间体6-氨基青霉烷酸(6-APA)的耗用量,收率从文献的70%提高到76%。中间体和最终产物的结构经1H-NMR确证。
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| 关 键 词： | 药物化学 工艺改进 化学合成 呋布西林钠 |
| 文章编号： | 1005-0108（2006）01-0051-03 |
| 收稿时间： | 2005-10-17 |
| 修稿时间： | 2005-10-17 |
Improved synthesis of furbenicillin sodium |
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| MA Yu-zhuo,LIU Ying-xiang,ZHOU Yu-ping,MEI Wen-jie,SHE Zhi-gang. Improved synthesis of furbenicillin sodium[J]. Chinese Journal of Medicinal Chemistry, 2006, 16(1): 51-53 |
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| Authors: | MA Yu-zhuo LIU Ying-xiang ZHOU Yu-ping MEI Wen-jie SHE Zhi-gang |
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| Affiliation: | 1. Department of Medicinal Chemistry, Guangdong Pharmaceutical University, Guangzhou 510006, China ; 2. College of Chemistryand Chemical Engineering, Sun Yat-Sen University, Guangzhou 510275, China |
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| Abstract: | Furbenicillin sodium,a known semi-synthetic ureide type of antibiotic firstly marketed in China,was synthesized from starting material 2-furaldehyde via six steps including oximation reaction,Beckmann rearrangement,isocyannuration,amination,condensation and salification etc.The synthetic process was improved by using sodium formate instead of sodium 2-ethylhexanoate and yield of the modified method was also raised to 76% with low consumption of 6-APA comparing with the 70% in the literature.The structures of all the intermediate and target compound were determined by ()~1H-NMR. |
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| Keywords: | medicinal chemistry process improvement chemical synthesis furbenicillin sodium |
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