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为了对盐酸尼洛替尼原料药的质量进行控制,合成了可能存在的5种有关物质:4-甲基-3-[[4-(3-吡啶基)-2-嘧啶基]氨基]苯甲酸(A)、4-甲基-N-[3-(4-乙基-1H-咪唑-1-基)-5-(三氟甲基)苯基]-3-[[4-(吡啶-3-基)嘧啶-2-基]氨基]苯甲酰胺(B),4-甲基-N-[3-(1H-咪唑-1-基)-5-(三氟甲基)苯基]-3-[[4-(吡啶-3-基)嘧啶-2-基]氨基]苯甲酰胺(C),4-甲基-N-[3-(2,4-二甲基-1H-咪唑-1-基)-5-(三氟甲基)苯基]-3-[[4-(吡啶-3-基)嘧啶-2-基]氨基]-苯甲酰胺(D),4-甲基-N-[3-(5-甲基-1H-咪唑-1-基)-5-(三氟甲基)苯基]-3-[[4-(吡啶-3-基)嘧啶-2-基]氨基]-苯甲酰胺(E),并经MS、~1H NMR确证结构。
In order to control the quality of nilotinib hydrochloride, five possible related substances were synthesized: 4-methyl-3- [4- (3-pyridyl) -2-pyrimidinyl] amino] benzene (A) 4-methyl-N- [3- (4-ethyl- 1 H- imidazol- 1 -yl) -5- (trifluoromethyl) phenyl] -3 - [[4- 3-yl) pyrimidin-2-yl] amino] benzamide (B) ] -3 - [[4- (pyridin-3-yl) pyrimidin- 2-yl] amino] benzamide (C) (D), 4 (pyridin-3-yl) pyrimidin-2-yl] amino] -benzamide (Trifluoromethyl) phenyl] -3 - [[4- (pyridin-3-yl) pyrimidine -2-yl] amino] -benzamide (E) and confirmed by MS, ~ 1H NMR.