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【结 构 式】

【药物名称】Eltrombopag, SB-497115-GR (as olamine), SB-497115, Promacta

【化学名称】3'-[2(Z)-[1-(3,4-Dimethylphenyl)-3-methyl-5-oxo-4,5-dihydro-1H-pyrazol-4-ylidene]hydrazino]-2'-hydroxybiphenyl-3-carboxylic acid

【CA登记号】496775-61-2, 376591-99-0 (as undefined isomer), 443130-00-5 (as undefined isomer hydrate), 496775-62-3 (as olamine)

【 分 子 式 】C25H22N4O4

【 分 子 量 】442.4667

【开发单位】GlaxoSmithKline (US); developed in collaboration with Ligand Pharmaceuticals, Inc. (US).

【药理作用】Antithrombocytopenic, Thrombopoietin receptor agonist

合成路线1

 

1 Duffy KJ, Erickson-Miller CL, Eppley DF, et al.2001. Thrombopoietin mimetics. WO 2001089457
2 Moore S. 2003. Preparation of (pyrazolidenehydrazino) [1,1'-biphenyl]-3-carboxylates as TPO receptor agonists for enhancing platelet prodn. WO 2003098992.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 20704 3-bromophenol 591-20-8 C6H5BrO 详情 详情
(II) 67115 2-Nitro-5-bromophenol;3-Bromo-6-nitrophenol;5-Bromo-2-nitrophenol 27684-84-0 C6H4BrNO3 详情 详情
(III) 67116 3'-hydroxy-4'-nitro-[1,1'-biphenyl]-4-carboxylic acid   C13H9NO5 详情 详情
(IV) 67117 4'-amino-3'-hydroxy-[1,1'-biphenyl]-4-carboxylic acid   C13H11NO3 详情 详情
(V) 67118 1-(3,4-dimethylphenyl)-3-methyl-1H-pyrazol-5(4H)-one 18048-64-1 C12H14N2O 详情 详情
(VI) 67119 3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid 496775-61-2 C25H22N4O4 详情 详情
(VII) 32841 4-(dihydroxyboryl)benzoic acid;4-Boronobenzoic acid;4-carboxyphenylboronic acid;4-(Dihydroxyboryl)benzoic acid 14047-29-1 C7H7BO4 详情 详情

合成路线2

 

1 Duffy KJ, Erickson-Miller CL, Eppley DF, et al.2001. Thrombopoietin mimetics. WO 2001089457
2 Moore S. 2003. Preparation of (pyrazolidenehydrazino) [1,1'-biphenyl]-3-carboxylates as TPO receptor agonists for enhancing platelet prodn. WO 2003098992.
中间体序号 中间体编号 品名 CAS号 分子式 供应商 用于合成
(I) 67120 2-Bromophenol;o-bromophenol 95-56-7 C6H5BrO 详情 详情
(II) 67121 2-bromo-6-nitrophenol 13073-25-1 C6H4BrNO3 详情 详情
(III) 67122 1-bromo-2-methoxy-3-nitrobenzene;1-bromo-2-methoxy-3-nitrobenzene 98775-19-0 C7H6BrNO3 详情 详情
(IV) 67124 2'-methoxy-3'-nitro-[1,1'-biphenyl]-3-carboxylic acid   C14H11NO5 详情 详情
(V) 67125 2'-hydroxy-3'-nitro-[1,1'-biphenyl]-3-carboxylic acid   C13H9NO5 详情 详情
(VI) 67126 3'-amino-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid 376592-93-7 C13H11NO3 详情 详情
(VII) 67118 1-(3,4-dimethylphenyl)-3-methyl-1H-pyrazol-5(4H)-one 18048-64-1 C12H14N2O 详情 详情
(VIII) 67119 3'-(2-(1-(3,4-dimethylphenyl)-3-methyl-5-oxo-1H-pyrazol-4(5H)-ylidene)hydrazinyl)-2'-hydroxy-[1,1'-biphenyl]-3-carboxylic acid 496775-61-2 C25H22N4O4 详情 详情
(IX) 67123 3-boronobenzoic acid   C7H7BO4 详情 详情
Extended Information