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奥拉帕利有关物质的合成

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以4-[3-(哌嗪-1-羰基)苄基]-2H-酞嗪-1 酮为原料,经与2-氟-5-[(4-氧代-3,4-二氢酞嗪-1 基)甲基]苯甲酸缩合,得到有关物质A;以4-[3-(哌嗪-1 羰基)苄基]-2H-酞嗪-1-酮为原料,经与丁酸缩合,得到有关物质B;以苯酞、3-氰基苯甲醛为原料,经亲核取代、氰基水解、肼解、酰胺化反应,得到有关物质C.这3种有关物质的制备方法和反应条件温和,操作简单,纯度高,其化学结构均经LR-EI-MS,1H-NMR和13C-NMR确证,可以用于奥拉帕利的质量研究和控制.
Synthesis of Related Substances of Olaparib
Related substance A was obtained by condensation of 4-[3-(piperazin-1-carbonyl)benzyl]-2H-phthalazin-1-one with 2-fluoro-5-[(4-oxo-3,4-dihydrophthalazin-1-yl)methyl]benzoic acid;related substance B was obtained by condensation of 4-[3-(piperazin-1-carbonyl)benzyl]-2H-phthalazin-1-one with butyric acid;related substance C was obtained from phthalide and 3-cyanobenzaldehyde via nucleophilic substitution,cyanohydrolysis,hydrazinolysis and amidation.These related substances were prepared under mild reaction conditions,simple operation and high purity,and their chemical structures were confirmed by LR-EI-MS,1H-NMR and 13C-NMR,which can be used for the quality study and control of olaparib.

olapribrelated substancessynthesisstructural characterization

李宏名、胡瑞馨、郑维江、张娇

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武汉轻工大学继续教育学院,湖北武汉 430023

国药集团川抗制药有限公司,四川成都 611731

四川农业大学园艺学院,四川成都 611130

四川科伦药物研究院有限公司,四川成都 611138

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奥拉帕利 有关物质 合成 结构确证

国家"重大新药创制"科技重大专项资助项目成都市高新区重点科技创新计划资助项目

2012ZX092021-01315DFZD023

2024

牡丹江师范学院学报(自然科学版)
牡丹江师范学院

牡丹江师范学院学报(自然科学版)

影响因子:0.426
ISSN:1003-6180
年,卷(期):2024.(1)
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