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| Synthesis of the Impurities of Dabigatran Etexilate Mesylate |
| GAO Hang1,3， ZONG Xin-jie2,3， CHEN Hui-hui3， LIU Chang-ying3， WANG Song-hui3， LI Chuan3， XU Wei-ren3 |
| 1. Graduate school, Tianjin Medical University, Tianjin 300070, China; 2. Graduate school, Tianjin University of Chinese Traditional Medicine, Tianjin 300193, China; 3. Tianjin Key Laboratory of Molecular Design and Drug Discovery， Tianjin Institute of Pharmaceutical Research Co., Ltd, Tianjin 300193, China |
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Abstract According to the synthetic route of dabigatran exetilate mesylate, seven kinds of impurities were synthesized: 3-【【【2-｛［(4-cyanophenyl)amino］methyl｝-1-methyl-1H-benzimidazol-5-yl】carbonyl】pyridin-2-ylamino】propionic acid(A), ethyl 3-【【【2-【｛［4-(ethoxy) tertiary amine］phenyl｝amino】methyl】-1-methyl-1H-benzimidazol-5-yl］carbonyl】pyridin-2-ylamino】propanoate hydrochlorid(B), ethyl 3-【【【2-【｛［(4-N′-methylcarbamimidoyl)phenyl］amino｝methyl】-1-methyl-1H-benzimidazol-5-yl】carbonyl】pyridin-2-ylamino】propanoate hydrochlorid(C), methyl 3-【【【2-【【【4-｛［(hexyloxy)carbonyl］carbamimidoyl｝phenyl】amino】methyl】-1-methyl-1H-benzimidazol-5-yl】carbonyl】(pyridin-2-yl)amino】propanoate hydrochlorid(D), ethyl 3-【【【2-【【【4-【｛［(hexyloxy)carbonyl］amino｝carbonyl】phenyl】amino】methyl】-1-methyl-1H-benzimidazol-5-yl】carbonyl】(pyridin-2-yl)amino】propanoate(E), 3-【【【2-【【【4-｛［(hexyloxy)carbonyl］carbamimidoyl｝phenyl】amino】methyl】-1-methyl-1H-benzimidazol-5-yl】-carbonyl】(pyridin-2-yl)amino】propanoic acid(F), ethyl (Z)-3-【【【2-【【【4-{［(N,N′-bishexyloxy)carbonyl］carbamimidoyl｝phenyl】amino】methyl】-1-methyl-1H-benzimidazol-5-yl】carbonyl】(pyridin-2-yl)amino】propanoate(G). The structures were confirmed by 1H NMR and ESI-MS.
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Received: 24 June 2015
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. [J]. Chinese Journal of Synthetic Chemistry, 2015, 23(12): 0-0. |
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2015, Vol. 23 
