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【结 构 式】

【药物名称】TPFA, Thiovir

【化学名称】Hydroxy(sulfanyl)phosphinecarboxylic acid oxide
      Thiophosphonoformic acid

【CA登记号】102805-86-7, 99107-93-4 (triNa salt)

【 分 子 式 】CH3O4PS

【 分 子 量 】142.07046

【开发单位】University of Southern California (Originator), Adventrx Pharmaceuticals (Licensee), National Cancer Institute (Codevelopment)

【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Anti-Papilloma Virus Drugs, Antiviral Drugs, Cervical Cancer Therapy, Genital Warts, Treatment for, Oncolytic Drugs, Reverse Transcriptase Inhibitors

合成路线1

The reaction of phosphonoformic acid trimethyl ester (I) with Lawesson's reagent in refluxing acetonitrile gives the thiophosphonate (II), which is hydrolyzed with 10 N NaOH.

1 McKenna, C.E.; Preparation and use of thiophosphonates and thio-analogues of phosphonoformic acid. US 5183812 .
2 McKenna, C.E.; Preparation and use of thiophosphonates and thio-analogues of phosphonoformic acid. US 5072032 .
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) 15993 Trimethyl phosphonoformate; Methyl dimethoxy(oxo)phosphoranecarboxylate 31142-23-1 C4H9O5P 详情 详情
(II) 64758 methyl bis(methyloxy)(thioxo)-lambda~5~-phosphanecarboxylate C4H9O4PS 详情 详情
Extended Information