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【结 构 式】

【分子编号】25122

【品名】2-amino-N-(3-[[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxy]methyl]-2,4-dichlorophenyl)-N-methylacetamide

【CA登记号】

【 分 子 式 】C18H17BrCl2N4O2

【 分 子 量 】472.16814

【元素组成】C 45.79% H 3.63% Br 16.92% Cl 15.02% N 11.87% O 6.78%

与该中间体有关的原料药合成路线共 1 条

合成路线1

该中间体在本合成路线中的序号:(IV)

Knoevenagel condensation of aldehyde (I) with malonic acid (II) provided substituted cinnamic acid (III). This was condensed with amino compound (IV) in the presence of 1-ethyl-3-(3-dimethylaminopropyl)carbodiimide.HCl (EDC) and 1-hydroxy-benzotriazole (HOBt) to give amide (V), which was then converted to the hydrochloride salt by reaction with methanolic HCl.

1 Abe, Y.; Kayakiri, H.; Satoh, S.; Inoue, T.; Sawada, Y.; Inamura, N.; Asano, M.; Hatori, C.; Sawai, H.; Oku, T.; Tanaka, H.; A novel class of orally active non-peptide bradykinin B2 receptor antagonists. 2. Overcoming the species difference between guinea pig and man. J Med Chem 1998, 41, 21, 4053.
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) 25120 4-formyl-N,N-dimethylbenzamide C10H11NO2 详情 详情
(II) 12963 Malonic acid 141-82-2 C3H4O4 详情 详情
(III) 25121 (E)-3-[4-[(dimethylamino)carbonyl]phenyl]-2-propenoic acid C12H13NO3 详情 详情
(IV) 25122 2-amino-N-(3-[[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxy]methyl]-2,4-dichlorophenyl)-N-methylacetamide C18H17BrCl2N4O2 详情 详情
(V) 25123 4-((E)-3-[[2-(3-[[(3-bromo-2-methylimidazo[1,2-a]pyridin-8-yl)oxy]methyl]-2,4-dichloromethylanilino)-2-oxoethyl]amino]-3-oxo-1-propenyl)-N,N-dimethylbenzamide C30H28BrCl2N5O4 详情 详情
Extended Information