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【结 构 式】 
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【药物名称】CYSTAZOSIN 【化学名称】N-[2-[2-[N-(4-Amino-6,7-dimethoxy-2-quinazolinyl)-Nmethylamino] ethyldisulfanyl]ethyl]-N-methylfurane-2- carboxamide 【CA登记号】 【 分 子 式 】C21H27N5O4S2 【 分 子 量 】477.60844 |
【开发单位】Recordati 【药理作用】PHARMACOLOGICAL TOOLS |
合成路线1
The monoacylation of disulfide (I) with 2-furylcarbonyl chloride (II) by means of 48% HBr in ethanol/water at 80 C gives the monoamide (III), which is then condensed with 2-chloro-6,7-dimethoxyquinazoline-4-amine (IV) in refluxing isoamyl alcohol.
| 【1】 Minarini, A.; Budriesi, R.; Chiarini, A.; Leonardi, A.; Melchiorre, C.; Search for alpha1-adrenoceptor subtypes selective antagonists: Design, synthesis and biological activity of cystazosin, an alpha1D-adrenoceptor antagonist. Bioorg Med Chem Lett 1998, 8, 11, 1353. |
| 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) | 26092 | N-methyl-2-[[2-(methylamino)ethyl]disulfanyl]-1-ethanamine; N-methyl-N-(2-[[2-(methylamino)ethyl]disulfanyl]ethyl)amine | C6H16N2S2 | 详情 | 详情 | |
| (II) | 26093 | 2-Furoyl chloride | 527-69-5 | C5H3ClO2 | 详情 | 详情 |
| (III) | 26094 | N-methyl-N-(2-[[2-(methylamino)ethyl]disulfanyl]ethyl)-2-furamide | C11H18N2O2S2 | 详情 | 详情 | |
| (IV) | 10143 | benzyl (2S)-2-aminopropanoate | C10H13NO2 | 详情 | 详情 |
Extended Information