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碱和水份对7-氯-6-氟-4-羟基喹啉-3-羧酸乙酯的N-或O-乙基化产物比例的影响
引用本文:郭惠元,孙兰英,曹一尘,田治明. 碱和水份对7-氯-6-氟-4-羟基喹啉-3-羧酸乙酯的N-或O-乙基化产物比例的影响[J]. 中国医药工业杂志, 1993, 0(7)
作者姓名:郭惠元  孙兰英  曹一尘  田治明
作者单位:中国医学科学院医药生物技术研究所 北京100050
摘    要:7-氯-6-氟-4-羟基喹啉-3-羧酸乙酯(3)的乙基化使用无水 K_2CO_3或无水 Na_2CO_3作脱酸剂,用HPLC 法测定 N-及 O-乙基化物(2与1)的相对含量。考察了溶剂中水份对2和1生成比例的影响。

关 键 词:诺氟沙星  合成中间体  喹啉衍生物

EFFECT OF DIFFERENT BASES AND HYDROUS SOLVENT ON RATIO OF N-AND O-ETHYLATED PRODUCTS OF ETHYL 7-CHLORO-6-FLUORO-4-HYDROXYQUINoUNE 3-CARBOXYLATE
GUO Hui-Yuan SUN Lan-Ying CAO Yi-Cheng TIAN Zhi-Ming. EFFECT OF DIFFERENT BASES AND HYDROUS SOLVENT ON RATIO OF N-AND O-ETHYLATED PRODUCTS OF ETHYL 7-CHLORO-6-FLUORO-4-HYDROXYQUINoUNE 3-CARBOXYLATE[J]. , 1993, 0(7)
Authors:GUO Hui-Yuan SUN Lan-Ying CAO Yi-Cheng TIAN Zhi-Ming
Abstract:Ethyl 7-chloro-6-fluoro-4-hydroxyquinoline-3-carboxylate (3) wassubjected to ethylation with ethyl bromide in different solvents (including hydrousDMF) with anhydrous K_2CO_3 or Na_CO_3 to give mixed N-and O-ethylated pro-ducts(2 and 1).The ratio betwean 2 and 1 in the mixture was investigated byHPLC method.The result indicated that the relative content of 1 was signifi-cantly reduced with Na_2CO_3 and not affected by the water contained in DMF.
Keywords:norfloxacin  synthesis  intermediate  quinoline derivative
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