普卢利沙星的合成 |
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引用本文: | 程春生,张宝砚,李鹏,杨贺选.普卢利沙星的合成[J].中国医药工业杂志,2005,36(2):67-69. |
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作者姓名: | 程春生 张宝砚 李鹏 杨贺选 |
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作者单位: | 1. 东北大学理学院,辽宁,沈阳,110000;沈阳化工研究院,辽宁,沈阳,110021 2. 东北大学理学院,辽宁,沈阳,110000 3. 沈阳化工研究院,辽宁,沈阳,110021 |
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摘 要: | 用3,4-二氟苯胺制得6,7-二氟-4-羟基-2-甲氧甲硫基喹啉-3-羧酸乙酯,在乙醇中与盐酸反应得到巯基化合物后,经与1,1-二碘乙烷环合、与哌嗪缩合、酸性水解得到6-氟-1-甲基-4-氧代-7-(1-哌嗪基)-1H,4H-1,3]硫氮杂环丁烷并3,2-a]喹啉-3-羧酸,最后与由3-羟基-2-丁酮和三光气反应后溴代得到的4-溴甲基-5-甲基-1,3-二噁环戊烯-2-酮缩合,得到氟喹诺酮类抗菌药普卢利沙星,总收率26%(以3,4-二氟苯胺计).
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关 键 词: | 普卢利沙星 抗菌药 合成 |
文章编号: | 1001-8255(2005)02-0067-03 |
Synthesis of Prulifloxacin |
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Authors: | CHENG Chun-Sheng ZHANG Bao-Yan LI Peng YANG He-Xuan |
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Affiliation: | CHENG Chun-Sheng1,2,ZHANG Bao-Yan1,LI Peng2,YANG He-Xuan2 |
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Abstract: | Prulifloxacin was synthesized from 3,4-difluoroaniline to afford ethyl 6,7-difluoro-4-hydroxy- 2-(methoxymethyl)thio]quinoline-3-carboxylate, which subjected to reaction with HCl in EtOH and subsequent to cyclizationwith1,1-diiodoethane,condensation withpiperazine,hydrolysisto give6-fluoro-1-methyl-4-oxo-7-(1-piperazinyl)- 1H,4H-1,3]-thiazeto3,2-a]quinoline-3-carboxylic acid, which followed by condensation with 4-bromomethyl-5-methyl- 1,3-dioxol-2-one. The overall yield was 24%(based on 3,4-difluoroaniline). |
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Keywords: | prulifloxacin antibacterial synthesis |
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