|
【结 构 式】 
|
【分子编号】19026 【品名】5-chloro-3-methoxy-2-pyrazinylamine; 5-chloro-3-methoxy-2-pyrazinamine 【CA登记号】 |
【 分 子 式 】C5H6ClN3O 【 分 子 量 】159.57496 【元素组成】C 37.63% H 3.79% Cl 22.22% N 26.33% O 10.03% |
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：(III)Bromination of 2-amino-5-chloropyrazine (I) with bromine in chloroform-pyridine provided bromopyrazine (II). Then, reaction with sodium methoxide in refluxing methanol afforded methyl ether (III). Finally, condensation of (III) with dansyl chloride (IV) in the presence of NaH in dimethoxyethane yielded the corresponding sulfonamide.
| 【1】 Hunt, S.J.; Tang, E.K.; James, R.; Heys, C.; Sumner, N.F.; Whiting, E.; Telford, B.; Dennis, M.; Mortlock, A.A.; Bath, C.; Wilson, C.; Butlin, R.J.; Bradbury, R.H.; New non-peptide endothelin-A receptor antagonists: Synthesis, biological properties, and structure-activity relationships of 5-(dimethylamino)-N-pyridyl-, -N-pyrimidinyl-, -N-pyridazinyl-, and -N-pyrazinyl-1-naphthalenesulfonamides. J Med Chem 1997, 40, 6, 996. |
| 【2】 Bradbury, R.H. (AstraZeneca plc); N-Heterocyclyl sulphonamide derivs. and their use as endothelin antagonists. EP 0752986; JP 1997510987; US 6083951; WO 9526957 . |
| 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) | 19024 | 5-chloro-2-pyrazinylamine; 5-chloro-2-pyrazinamine | C4H4ClN3 | 详情 | 详情 | |
| (II) | 19025 | 3-bromo-5-chloro-2-pyrazinylamine; 3-bromo-5-chloro-2-pyrazinamine | C4H3BrClN3 | 详情 | 详情 | |
| (III) | 19026 | 5-chloro-3-methoxy-2-pyrazinylamine; 5-chloro-3-methoxy-2-pyrazinamine | C5H6ClN3O | 详情 | 详情 | |
| (IV) | 19027 | 5-(dimethylamino)-1-naphthalenesulfonyl chloride | 605-65-2 | C12H12ClNO2S | 详情 | 详情 |
Extended Information