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丁酸氯维地平中杂质化合物的合成

Synthesis of Impurity Compounds in Preparation of Generic Clevidipine Butyrate

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【作者】 夏万东沈国兵关荐伊

【Author】 XIA Wan-dong;SHEN Guo-bing;GUAN Jian-yi;Chengde Petroleum College;Taiyuan University of Technology;

【机构】 承德石油高等专科学校太原理工大学

【摘要】 为建立丁酸氯维地平药物的仿制提供了杂质标准品,对其4个特定杂质进行合。以2,3-二氯苯甲醛、乙酰乙酸(2-氰基)乙酯、3-氨基巴豆酸甲酯、乙酰乙酸甲酯和三羟基丙腈为主要试剂,制备了丁酸氯维地平4个杂质:4-(2,3-二氯苯基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸单甲酯,6-(2,3-二氯苯基)-2-甲基-4-氧代环己烯-2-甲酸甲酯,6-(2,3-二氯苯基)-4-甲基-2-氧代环己烯-3-甲酸甲酯,4-(2,3-二氯苯基)-2,6-二甲基-1,4-二氢吡啶-3,5-二羧酸甲基酯。所合成的杂质结构经NMR和MS确证,杂质的含量达到98%。

【Abstract】 For providing impurity standard of clevidipine butyrate generic drug,four specific compounds were synthesized.With 2,3-dichlorobenzaldehyde,ethyl 2-cyanoacetoacetate,methyl 3-aminocrotonate,methyl acetoacetate and 3-hydroxypropionitrile as main reagents 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid monomethyl ester, 6-(2,3-dichlorophenyl)-2-methyl-4-oxocyclohexene-2-carboxylate,6-(2,3-dichlorophenyl)-4-methyl-2-oxo-cyclohexen-3-carboxylate,and 4-(2,3-dichlorophenyl)-2,6-dimethyl-1,4-dihydropyridine-3,5-dicarboxylic acid methyl ester were prepared.The structure of the synthesized compounds was confirmal by NMR and MS,and their purity reached 98%.

【关键词】 丁酸氯维地平杂质合成表征
【Key words】 clevidipine butyrateimpuritiessynthesischaracterization
  • 【分类号】TQ460.6
  • 【被引频次】1
  • 【下载频次】124
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