2-氟-5-[(4-氧代-3,4-二氢酞嗪-1-基)甲基]苯甲酸的合成工艺改进
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  • 英文篇名:Improved Synthesis of 2-fluoro-5-[(4-oxo-3h-phthalazin-1-yl)methyl]Benzoic acid
  • 作者:陈升 ; 陈绘如
  • 英文作者:Chen Sheng;Chen Huiru;Fujian Architectural Institute of technology;Changzhou Institute of Engineering Technology;
  • 关键词:2-氟-5-[(4-氧代-3 ; 4-二氢酞嗪-1-基)甲基]苯甲酸 ; 奥拉帕尼中间体 ; 合成
  • 英文关键词:2-fluoro-5-[(4-oxo-3h-phthalazin-1-yl) methyl]Benzoic;;acidolaparib;;intermediatesynthesis
  • 中文刊名:HGJS
  • 英文刊名:Chemical Industry Times
  • 机构:福建建筑学校;常州工程职业技术学院;
  • 出版日期:2018-03-30
  • 出版单位:化工时刊
  • 年:2018
  • 期:v.32;No.369
  • 语种:中文;
  • 页:HGJS201803006
  • 页数:3
  • CN:03
  • ISSN:32-1320/TQ
  • 分类号:20-22
摘要
使用较为价廉的邻苯二甲酰亚胺作为起始原料,经选择性还原、加成、水解,合成了目标化合物2-氟-5-[(4-氧代-3,4-二氢酞嗪-1-基)甲基]苯甲酸,总收率达60.5%。相应各步反应条件得以优化,用质谱、核磁共振氢谱确定了目标化合物的结构。该方法起始原料价廉易得,操作简单易行,具有工业化应用前景。
        2-fluoro-5-[(4-oxo-3 h-phthalazin-1-yl) methyl]Benzoic acid was synthesized by condensing Phthalimide,and followed by reduction,addition reaction,hydrolysisformation. The total yield was 60. 5%.Structures of the target product were verified by MS and ~1HNMR. The reaction condition was mild. The optimum synthetic procedure was synthesized with materials of lower cost,and was suitable for industrial production.
引文
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