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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。
In order to control the quality of the imatinib mesylate product, five related substances contained in the quality standard were synthesized: 4 - [(piperazin-1-yl) methyl] -N- [4- Amino] phenyl] benzamide (A), 4 - [(4-methyl-1,4-dioxopiperazin-1-yl) Methyl] -N- [4-methyl-3- [[4- (3- pyridyl) pyrimidin-2-yl] amino] phenyl] benzamide (B) (4-methyl-3- [[4- (3-pyridyl) pyrimidin-2-yl] amino] phenyl] benzamide ( (4-Methyl-4-oxopiperazin- 1 -yl) methyl] -N- [4-methyl-3- [[4- (3-pyridyl) pyrimidin-2- Amino] phenyl] benzamide (D) and 1,4-bis [4- [4-methyl- 3- [[4- (3- pyridyl) pyrimidin- 2-yl] amino] ] Carbamoyl] benzylpiperazine (E), confirmed by ~ 1H NMR, MS and other structures.