One-pot synthesis of aryl phosphoramidate derivatives of AZT/d4T as anti-HIV prodrugs

被引：5
|
作者：
Jiang, P
Guo, J
Fu, H [1 ]
Jiang, YY
Zhao, YF
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, Guangdong Prov Grad Sch Shenzhen, Key Lab Chem Biol, Shenzhen 518057, Peoples R China
来源：
SYNLETT | 2005年 / 16期
关键词：
aryl phosphoramidate derivatives; anti-HIV prodrugs; N-chlorosuccinimide (NCS); AZT; d4T;
D O I：
10.1055/s-2005-917085
中图分类号：
O62 [有机化学];
学科分类号：
070303 ; 081704 ;
摘要：
Arbuzov reaction of aryl phosphorodichloridite with mixture of one equivalent of AZT or d4T and one equivalent of tertbutyl alcohol led to the corresponding AZT/d4T aryl H-phosphonate diesters. and the following reaction of the H-phosphonate diesters with amino acid methyl esters in the presence of N-chloro-succinimide (NCS) produced membrane-soluble anti-HIV prodrugs AZT/d4T aryl phosphoramidate derivatives in good yields.
引用
收藏
页码：2537 / 2539
页数：3
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