New and efficient approach to aryl phosphoramidate derivatives of AZT/d4T as anti-HIV prodrugs

被引:13
|
作者
Li, XS
Fu, H [1 ]
Jiang, YY
Zhao, YF
Liu, JY
机构
[1] Tsing Hua Univ, Dept Chem, Minist Educ, Key Lab Bioorgan Phosphorous Chem & Chem Biol, Beijing 100084, Peoples R China
[2] Tsing Hua Univ, Coll Shenzhen, Key Lab Chem Biol, Shenzhen 518057, Peoples R China
关键词
aryl phosphoramidate; anti-HIV; AZT; d4T;
D O I
10.1055/s-2004-834800
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Ester exchange of diaryl phosphite with AZT or d4T produced aryl AZT/d4T H-phosphonate, and the following reaction with amino acid esters in the presence of hexachloroethane and triethylamine yielded membrane-soluble anti-HIV prodrugs aryl phosphoramide derivatives of AZT and d4T in good yields.
引用
收藏
页码:2600 / 2602
页数:3
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