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【结 构 式】 
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【药物名称】DDE-240, F-PBT, HI-240 【化学名称】N-(5-Bromo-2-pyridinyl)-N'-[2-(2-fluorophenyl)ethyl]thiourea 【CA登记号】219664-37-6 【 分 子 式 】C14H13BrFN3S 【 分 子 量 】354.24621 |
【开发单位】Parker Hughes Institute (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Contraceptives, Disorders of Sexual Function and Reproduction, Treatment of, ENDOCRINE DRUGS, Female Contraceptives, Vaginal Spermicides, Reverse Transcriptase Inhibitors |
合成路线1
2-Amino-5-bromopyridine (I) was condensed with 1,1-thiocarbonyldiimidazole (II) in acetonitrile to furnish the precursor thiocarbonyl derivative (III). Further reaction of (III) with 2-fluorophenethylamine (IV) in DMF at 100 C gave the target thiourea.
| 【1】 Vig, R.; Mao, C.; Venkatachalam, T.K.; Tuel-Ahlgren, L.; Sudbeck, E.A.; Uckun, F.M.; Rational design and synthesis of phenethyl-5-bromopyridyl thiourea derivatives as potent non-nucleoside inhibitors of HIV reverse transcriptase. Bioorg Med Chem 1998, 6, 10, 1789. |
| 【2】 Uckun, F.M. (Parker Hughes Institute); NNI for treatment of multi-drug resistant HIV. WO 0056736 . |
| 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) | 26465 | methyl (2S,3R)-3-cyclopropyl-2,3-dihydroxypropanoate | C7H12O4 | 详情 | 详情 | |
| (IV) | 31333 | 2-fluorophenethylamine; 2-(2-fluorophenyl)-1-ethanamine | C8H10FN | 详情 | 详情 |
Extended Information