| 氟哌酸中间体—3-氯-4-氟苯胺亚甲基丙二酸二乙酯的合成工艺改进 |
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| 引用本文： | 朱崇泉,郭争鸣,边军,吴国沛. 氟哌酸中间体—3-氯-4-氟苯胺亚甲基丙二酸二乙酯的合成工艺改进[J]. 中国药物化学杂志, 1991, 0(2) |
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| 作者姓名： | 朱崇泉 郭争鸣 边军 吴国沛 |
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| 作者单位： | 南京药物研究所，南京药物研究所，南京药物研究所，南京药物研究所 南京 210009，南京 210009，南京 210009，南京 210009 |
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| 摘 要： | 3-氯-4-氟苯胺在适当的Lewis酸存在下,与原甲酸三乙酯及丙二酸二乙酯缩合,一步制得了3-氯-4-氟苯胺亚甲基丙二酸二乙酯(Ⅲ),反应收率几乎为100％,本方法可在氟哌酸的生产巾完全代替乙氧_亚甲基丙二酸二乙酯工艺。
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| 关 键 词： | 3-氯-4-氟苯胺亚甲基丙二酸二乙酯 氟哌酸 合成 |
IMPROVED SYNTHESIS OF DIETHYL 3-CHLORO-4-FLUORO-ANILINOMETHYLENEMALONATE |
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| Zhu Chongquan Guo Zhengming Bian Jun Wu Guopei. IMPROVED SYNTHESIS OF DIETHYL 3-CHLORO-4-FLUORO-ANILINOMETHYLENEMALONATE[J]. Chinese Journal of Medicinal Chemistry, 1991, 0(2) |
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| Authors: | Zhu Chongquan Guo Zhengming Bian Jun Wu Guopei |
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| Abstract: | The diethyl 3-chloro-4-fluoro-anilinomethylenemalonate was synthesized within one step by condensation of 3-chloro-4-fluoro-aniline with triethyl orthoformate and diethyl malonate in an appropriate molecular ratio and in the presence of an appropriate Lewis acid.The yield of this condensation was almost 100%. Thus the method could be used in the synthesis of Norfloxacin instead of that of the condensation of diethyl ethoxylmethylene malonate and 3-chloro-4-fluoro-aniline. |
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| Keywords: | Diethyl 3-chloro-4-fluoro-anilinomothylenemalonate Synthesis |
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