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【结 构 式】 
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【药物名称】 【化学名称】6-Fluoro-9-[1-(hydroxymethyl)-2-(isobutyryloxy)ethoxymethyl]purine-2-amine 【CA登记号】 【 分 子 式 】C13H18FN5O4 【 分 子 量 】327.31791 |
【开发单位】SK Pharma (Licensee) 【药理作用】AIDS Medicines, ANTIINFECTIVE THERAPY, Antiviral Drugs, Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems, Treatment of Opportunistic Infections |
合成路线1
Treatment of 6-deoxy-6-chloroganciclovir (I) with trimethylamine in DMF-THF at low temperature produced the trimethylammonium salt (II), which was subsequently displaced with KF in DMF at 80 C under vacuum removal of the Me3N to afford the corresponding 6-fluoro derivative (III). Finally, monoacylation with one equivalent of isobutyric anhydride (IV) in the presence of DMAP provided the target ester.
| 【1】 Kim, D.-K.; Chang, K.; Im, G.-J.; Kim, H.-T.; Lee, N.; Kim, K.H.; Synthesis and evaluation of 2-amino-9-(1,3-dihydroxy-2-propoxymethyl)-6-fluoropurine mono- and diesters as potential prodrugs of ganciclovir. J Med Chem 1999, 42, 2, 324. |
| 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) | 22331 | 2-[(2-amino-6-chloro-9H-purin-9-yl)methoxy]-1,3-propanediol | C9H12ClN5O3 | 详情 | 详情 | |
| (II) | 22332 | 2-[[2-amino-6-(trimethyl-lambda(5)-azanyl)-9H-purin-9-yl]methoxy]-1,3-propanediol | C12H22N6O3 | 详情 | 详情 | |
| (III) | 22333 | 2-[(2-amino-6-fluoro-9H-purin-9-yl)methoxy]-1,3-propanediol | C9H12FN5O3 | 详情 | 详情 | |
| (IV) | 22334 | 1-methylpropionic anhydride | 97-72-3 | C8H14O3 | 详情 | 详情 |
Extended Information