【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