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【结 构 式】 
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【药物名称】Foscarnet sodium, EHB-776, PFA, A-29622, Triapten, Virudin, Foscavir 【化学名称】Phosphonoformic acid trisodium salt 【CA登记号】63585-09-1 【 分 子 式 】CNa3O5P 【 分 子 量 】191.95135 |
【开发单位】AstraZeneca (Originator), Wyeth Pharmaceuticals (Not Determined), Bracco (Licensee), Merck & Co. (Licensee) 【药理作用】Anti-Cytomegalovirus Drugs, Anti-Herpes Virus Drugs, ANTIINFECTIVE THERAPY, Antiviral Drugs, Reverse Transcriptase Inhibitors |
合成路线1
The reduction of triethyl phosphite (I) with ethyl chloroformate (II) gives phosphonoformic acid triethyl ester (III), which is hydrolyzed with refluxing aqueous NaOH. Other alkyl esters can be used instead.
| 【1】 McIntosh, C.L.; Carboxyphosphonates. US 4018854 . |
| 【2】 McIntosh, C.L.; Carboxyphosphonate brush control agents. US 4042650 . |
| 【3】 Castaner, J.; Blancafort, P.; Hopkins, S.J.; Serradell, M.N.; Foscarnet sodium. Drugs Fut 1980, 5, 7, 345. |
| 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) | 15487 | triethyl phosphite | 122-52-1 | C6H15O3P | 详情 | 详情 |
| (II) | 11229 | 1-[(Chlorocarbonyl)oxy]ethane;ethyl carbonochloridate; Carbonchloridic acid ethyl ester;Ethyl chloroformate;Ethyl chlorocarbonate | 541-41-3 | C3H5ClO2 | 详情 | 详情 |
| (III) | 32722 | Ethyl diethoxy(oxo)phosphoranecarboxylate; Phosphonoformic acid triethyl ester | 1474-78-8 | C7H15O5P | 详情 | 详情 |