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【结 构 式】 
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【药物名称】GP-49 【化学名称】N-(5-Chloropyridin-2-yl)-N'-[2-(2,6-difluorophenyl)ethyl]thiourea 【CA登记号】149487-93-4 【 分 子 式 】C14H12ClF2N3S 【 分 子 量 】327.78564 |
【开发单位】Medivir (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Reverse Transcriptase Inhibitors |
合成路线1
2,6-Difluorophenethylamine (II) was prepared by reduction of nitrile (I) with either NaBH4 in the presence of CoCl2 or borane in THF. Reaction of amine (II) with thiocarbonyldiimidazole (III) furnished the thioimidazolide (IV). This was finally condensed with 2-amino-5-chloropyridine (V), yielding the corresponding thiourea.
| 【1】 Lind, P.T.; Noreen, R.; Ternansky, R.J.; Morin, J.M. Jr. (Medivir AB); Cpds. and methods for inhibition of HIV and related viruses. WO 9303022 . |
| 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) | 46429 | 2-(2,6-difluorophenyl)acetonitrile | C8H5F2N | 详情 | 详情 | |
| (II) | 46430 | 2-(2,6-difluorophenyl)-1-ethanamine; 2,6-difluorophenethylamine | C8H9F2N | 详情 | 详情 | |
| (III) | 11990 | Di(1H-imidazol-1-yl)methanethione; 1,1'-Thiocarbonyldiimidazole | 6160-65-2 | C7H6N4S | 详情 | 详情 |
| (IV) | 46431 | N-(2,6-difluorophenethyl)-1H-imidazole-1-carbothioamide | C12H11F2N3S | 详情 | 详情 | |
| (V) | 18559 | 5-Chloro-2-pyridinylamine; 5-Chloro-2-pyridinamine; 2-Amino-5-chloropyridine | 1072-98-6 | C5H5ClN2 | 详情 | 详情 |
Extended Information