【结 构 式】 |
【药物名称】 【化学名称】3'-Azido-3'-deoxy-5'-O-(4-hydroxybutyloxycarbonyl)thymidine 【CA登记号】313343-81-6 【 分 子 式 】C15H21N5O7 【 分 子 量 】383.36392 |
【开发单位】Laphal (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Chemical Delivery Systems, DRUG DELIVERY, Drug Delivery Systems |
合成路线1
The desired product can be obtained by condensation of commercial AZT (I) with N,N’-carbonyldiimidazole (CDI) in DMF followed by treatment with 1,4-butanediol (II) in the same solvent.
【2】 Vlieghe, P.; Bihel, F.; Clerc, T.; et al.; New 3'-azido-3'-deoxythymidin-5'-yl O-(omega-hydroxyalkyl) carbonate prodrugs: Synthesis and anti-HIV evaluation. J Med Chem 2001, 44, 5, 777. |
【3】 Kraus, J.-L.; Clerc, T.; Salles, J.-P.; Vlieghe, P. (Laboratoires Laphal); Novel cpds. derived from nucleosides, preparation methods and pharmaceutical compsns. containing same. FR 2794752; WO 0077020 . |
【4】 Vlieghe, P.; Salles, J.-P.; Clerc, T.; Kraus, J.-L. (Laboratoires Laphal); Novel esters derived from nucleosides, preparation methods and pharmaceutical compsns. containing them. FR 2796384; WO 0104134 . |
【1】 Clerc, T.; Pannecouque, C.; Vlieghe, P.; Kraus, J.-L.; Salles, J.-P.; De Clercq, E.; Witvrouw, M.; New 3'-azido-3' deoxythymidin-5'-yl O-(4-hydroxyalyl or -alkenyl or -alkylepoxide) carbonate prodrugs: Synthesis and anti-HIV evaluation. J Med Chem 2001, 44, 18, 3014. |
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