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【结 构 式】 
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【药物名称】HI-443 【化学名称】N-(5-Bromopyridin-2-yl)-N'-[2-(2-thienyl)ethyl]thiourea 【CA登记号】258340-15-7 【 分 子 式 】C12H12BrN3S2 【 分 子 量 】342.28154 |
【开发单位】Parker Hughes Institute (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Reverse Transcriptase Inhibitors |
合成路线1
Reaction of 2-amino-5-bromopyridine (I) with thiocarbonyl diimidazole (II) provided the thioimidazolide (III). This was then coupled with 2-(2-thienyl)ethyl amine (IV) to furnish the target thiourea.
| 【1】 Maher, D.; Mao, C.; Tuel-Ahlgren, L.; Uckun, F.M.; Zhu, D.; Pendergrass, S.; Venkatachalam, T.K.; N'-[2-(2-Thiophene)ethyl]-N'-[2-(5-bromopyridyl)] thiourea as a potent inhibitor of NNI-resistant and multidrug-resistant human immunodeficiency virus-1. Bioorg Med Chem Lett 1999, 9, 24, 3411. |
| 【2】 Ventatachalam, T.K.; Uckun, F.M. (Parker Hughes Institute); Thiophene-ethyl thiourea cpds. and use. US 6124324; WO 0078755 . |
| 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) | 12123 | 5-Bromo-2-pyridinylamine; 5-Bromo-2-pyridinamine; 2-Amino-5-bromopyridine | 1072-97-5 | C5H5BrN2 | 详情 | 详情 |
| (II) | 11990 | Di(1H-imidazol-1-yl)methanethione; 1,1'-Thiocarbonyldiimidazole | 6160-65-2 | C7H6N4S | 详情 | 详情 |
| (III) | 24645 | N-(5-bromo-2-pyridinyl)-1H-imidazole-1-carbothioamide | C9H7BrN4S | 详情 | 详情 | |
| (IV) | 35253 | 2-(2-thienyl)ethylamine; 2-(2-thienyl)-1-ethanamine; 2-Thiophene ethylamine | 30433-91-1 | C6H9NS | 详情 | 详情 |
Extended Information