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【结 构 式】 
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【药物名称】SO-730 【化学名称】5'-O-[(O-Benzyl-L-alanino)(phenoxy)phosphoryl]-3'-deoxy-2',3'-didehydrothymidine 【CA登记号】178469-24-4 【 分 子 式 】C26H28N3O8P 【 分 子 量 】541.50216 |
【开发单位】Rega Institute for Medical Research (Originator) 【药理作用】AIDS Medicines, Anti-HIV Agents, ANTIINFECTIVE THERAPY, Antiviral Drugs |
合成路线1
Title phosphoramidate was obtained by condensation of phenyl (benzyloxyalanino)phosphorochloridate (I) with 2',3'-dideoxy-2',3'-didehydrothymidine (II) in the presence of N-methylmorpholine in THF at r.t.
| 【1】 Balzarini, J.; De Clercq, E.; Sheeka, H.M.; Cahard, D.; McGuigan, C.; Phosphoramidate derivatives of d4T with improved anti-HIV efficacy retain full activity in thymidine kinase-deficient cells. Bioorg Med Chem Lett 1996, 6, 10, 1183. |
| 【2】 McGuigan, C.; Sutton, P.W.; Cahard, D.; Turner, K.; O'Leary, G.; Wang, Y.; Gumbleton, M.; De Clercq, E.; Balzarini, J.; Synthesis, anti-human immunodeficiency virus activity and esterase lability of some novel carboxylic ester-modified phosphoramidate derivatives of stavudine (d4T). Antivir Chem Chemother 1998, 9, 6, 473. |
Extended Information