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| 6,7-二氟-4-羟基-2-甲氧甲硫基-3-喹啉羧酸乙酯的合成 | |
| 引用本文： | 程春生,张宝砚,李鹏,杨贺选.6,7-二氟-4-羟基-2-甲氧甲硫基-3-喹啉羧酸乙酯的合成[J].中国医药工业杂志,2004,35(8):459-460. |
| 作者姓名： | 程春生 张宝砚 李鹏 杨贺选 |
| 作者单位： | 1. 东北大学理学院,辽宁,沈阳,110004;沈阳化工研究院,辽宁,沈阳,110021 2. 东北大学理学院,辽宁,沈阳,110004 3. 沈阳化工研究院,辽宁,沈阳,110021 |
| 摘 要： | 3,4-二氟苯胺在三乙胺存在下与二硫化碳生成芳基取代的二硫代氨基甲酸后与氯甲酸乙酯反应得到3,4-二氟苯基异硫氰酸酯,先后与由丙二酸二乙酯在无机碱中成的盐和氯甲基甲醚反应后加热环合,得到氟喹诺酮类抗菌剂普卢利沙星的中间体6,7-二氟-4-羟基-2-甲氧甲硫基-3-喹啉羧酸乙酯,总收率85.7%. |
| 关 键 词： | 6 7-二氟-4-羟基-2-甲氧甲硫基-3-喹啉羧酸乙酯 普卢利沙星 氟喹诺酮 抗菌剂 中间体 合成 |
| 文章编号： | 1001-8255(2004)08-0459-02 |
Synthesis of Ethyl 6,7-Difluoro-4-hydroxy-2- [(methoxymethyl) thio]- quinoline-3-carboxylate |
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| Authors: | CHENG Chun-Sheng ZHANG Bao-Yan LI Peng YANG He-Xuan |
| Institution: | CHENG Chun-Sheng1,2,ZHANG Bao-Yan1,LI Peng2,YANG He-Xuan2 |
| Abstract: | Ethyl 6,7-difluoro-4-hydroxy-2-(methoxymethyl)thio]quinoline- 3-carboxylate, a key intermediate ofprulifloxacin, was synthesized by treatment of 3,4-difluoroaniline with carbon disulfide in the presence of triethylamine andthen reacted with ethyl chloroformate to give 3,4-difluorophenylisothiocyanate, which reacted successively with diethylmalonate in the presence of KOH and chloromethyl methyl ether and then cyclization with an overall yield of 85.7%. |
| Keywords: | ethyl 6 7-difluoro-4-hydroxy-2-[(methoxymethyl)thio]quinoline- 3-carboxylate prulifloxacin fluoroquinolone antibacterial agent intermediate synthesis |
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