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4(R)—(6—氨基—9H—嘌呤—9—基)—2(R)—(羟甲基)四氢呋喃—3(R)—醇的合成
引用本文:赵桂森 NairV. 4(R)—(6—氨基—9H—嘌呤—9—基)—2(R)—(羟甲基)四氢呋喃—3(R)—醇的合成[J]. 中国药学, 2000, 9(3): 137-141
作者姓名:赵桂森 NairV
作者单位:[1]山东医科大学药物化学教研室,济南250012 [2]DepartmentofChemistrty,TheUniversityofIowa,U.S.A.
摘    要:为寻找抗HIV化合物,我们以D-核糖为原料,经甲基化、硅烷基化、还原裂解反应制得重要中间体1-脱氧核糖(5),再通过形成环状亚砜化合物,与NaN3发生反应后,经过还原、缩合、环合、氨化、脱保护基反应制得异脱氧腺嘌呤核苷(1),各步反应收率均超过70%。其抗HIV活性测定尚在进行中。

关 键 词:核苷 异脱氧腺嘌呤核苷 抗病毒化合物 合成

Synthesisof4(R)-(6-Amino-9H-Purine-9-yl)-2(R)-(Hydroxymethyl) tetrahydrofuran-3(R)-ol
Zhao Guisen. Synthesisof4(R)-(6-Amino-9H-Purine-9-yl)-2(R)-(Hydroxymethyl) tetrahydrofuran-3(R)-ol[J]. Journal of Chinese Pharmaceutical Sciences, 2000, 9(3): 137-141
Authors:Zhao Guisen
Affiliation:Zhao Guisen 1 1. Department of Medicinal Chemistry,Shandong Medical University,Jinan 250012, Vasu Nair 2 2. Department of Chemistry,the University of Iowa,U.S.A.
Abstract:1-Deoxyribose (5), prepared from D-ribose via methylation, silylation and reductive cleavage, was converted into cyclic sulfite(7). Reaction of 7 with NaN3 resulted in azide (8), which was converted to the isomeric deoxy adenosine, 4(R)-(6-amino-9H-purin-9-yl)-2(R)-(hydroxymethyl) tetrahy-drofuran- 3(R)-ol (1) by a sequence of five high-yield reactions. Antiviral studies are in progress.
Keywords:Nucleoside  Isodeoxyadenosine  Antiviral agent  Synthesis
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