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甲磺酸伊马替尼有关物质的合成
引用本文:吴立红,何元,张彦巧,张素娟,王宝玮. 甲磺酸伊马替尼有关物质的合成[J]. 中国医药工业杂志, 2011, 42(10)
作者姓名:吴立红  何元  张彦巧  张素娟  王宝玮
作者单位:石药集团药物研究院,河北石家庄,050051
摘    要:为了控制甲磺酸伊马替尼产品质量,分别合成了质量标准所载的5种有关物质:4-[(哌嗪-1-基)甲基]-N-[4-甲基-3-[ [4- (3-吡啶基)嘧啶-2-基]氨基]苯基]苯甲酰胺(A),4-[(4-甲基-1,4-二氧化哌嗪-1-基)甲基]-N-[4-甲基-3-[ [4- (3-吡啶基)嘧啶-2-基]氨基]苯基]苯甲酰胺(B),4-[(4-甲基-1-氧化哌嗪-1-基)甲基]-N-[4-甲基-3-[ [4- (3-吡啶基)嘧啶-2-基]氨基]苯基]苯甲酰胺(C),4-[ (4-甲基-4-氧化哌嗪-1-基)甲基]-N-[4-甲基-3-[ [4- (3-吡啶基)嘧啶-2-基]氨基]苯基]苯甲酰胺(D)和1,4-双[4-[4-甲基-3-[ [4- (3-吡啶基)嘧啶-2-基]氨基]苯基]氨甲酰基]苄基哌嗪(E),并经1H NMR、MS等确证结构.

关 键 词:甲磺酸伊马替尼  有关物质  合成

Synthesis of Related Substances of Imatinib Mesylate
WU Lihong,HE Yuan,ZHANG Yanqiao,ZHANG Sujuan,WANG Baowei. Synthesis of Related Substances of Imatinib Mesylate[J]. , 2011, 42(10)
Authors:WU Lihong  HE Yuan  ZHANG Yanqiao  ZHANG Sujuan  WANG Baowei
Affiliation:WU Lihong,HE Yuan,ZHANG Yanqiao,ZHANG Sujuan,WANG Baowei (Pharmaceutical Research Institute of Shijiazhuang Pharmaceutical Group Co.,Ltd.,Shijiazhuang 050051)
Abstract:To perform the quality control of imatinib mesylate,five related substances recorded in quality standard were prepared,and their structures were confirmed by ~1H NMR and MS.These substances were 4-[(piperazin-1-yl)methyl]-N-[4-methyl-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino]phenyl]benzamide(A), 4-[(4-methyl-1,4-dioxidopiperazin-1-yl)methyl]-N-[4-methyl-3-[[4-(pyridin-3-yl)pyrimidin-2-yl]amino] phenyl]benzamide(B),4-[(4-methyl-1-oxidopiperazin-1-yl) methyl]-N-[4-methyl-3-[[4-(pyridin-3-yl) pyrimidin-2 -yl]am...
Keywords:imatinib mesylate  related substance  synthesis  
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