2′,3′-乙氧甲撑基腺苷5′-硫代磷酰氨基酸酯的合成和谱学分析  

Synthesis and Spectroscopic Analysis of 2′,3′-O-Ethoxymethylidene Adenosine 5′-Thiophosphoramidates

作　　者：苗志伟[1] 冯玉萍[1] 付华[1] 涂光忠[2] 赵玉芬[1] 

机构地区：[1]清华大学化学系,教育部生命有机磷化学重点实验室,北京100084 [2]北京微量化学研究所,北京100091

出　　处：《高等学校化学学报》2002年第12期2284-2286,共3页Chemical Journal of Chinese Universities

基　　金：国家自然科学基金 (批准号 :2 990 2 0 0 3;39870 415 );清华大学博士生创新基金 (批准号 :0 92 430 30 5 )资助

摘　　要：Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.Nucleoside reverse transcriptase inhibitors are the only drugs so far approved for the treatment of AIDS. Several nucleoside analogs are potent inhibitors of human immunodeficiency virus(HIV) in cell culture. However, in many cases the nucleoside derivatives have a poor affinity for nucleoside kinases. Nucleoside 5′-phosphorothioates is relatively resistant to enzymatic transformations. In this paper, 2′,3′-O-alkoxymethylidene adenosine 5′-thiophosphoramidates were synthesized through a highly efficient approach. The new compounds were characterized by NMR, IR and ESI-MS.

关 键 词：2' 3’-乙氧甲撑基腺苷5'-硫代磷酰氨基酸酯 合成 谱学分析 抗艾滋病药物 抗HIV-1药物活性 

分 类 号：R512.91[医药卫生—内科学] R914[医药卫生—临床医学]