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具有腺嘌呤和胸腺嘧啶碱基部分的3'-O-膦酰基乙基核苷的合成。

Synthesis of 3'-o-phosphonoethyl nucleosides with an adenine and a thymine base moiety.

作者信息

Huang Qiuya, Herdewijn Piet

机构信息

Laboratory of Medicinal Chemistry, Rega Institute for Medical Research, K.U. Leuven, Leuven, Belgium.

出版信息

Nucleosides Nucleotides Nucleic Acids. 2009 May;28(5):337-51. doi: 10.1080/15257770903044184.

DOI:10.1080/15257770903044184
PMID:20183588
Abstract

The synthesis and antiviral evaluation of new 3'-O-phosphonoethyl modified phosphonate nucleosides related to PMDTA and PMDTT is described. The reaction scheme starts from protected L-threose and the phosphonate group is introduced by the Arbuzov reaction. The 2'-OH as well as the 2'-deoxygenated nucleosides have been obtained. Unfortunately, none of these synthesized compounds shows activity against HIV and HCV.

摘要

描述了与PMDTA和PMDTT相关的新型3'-O-膦酰基乙基修饰的膦酸酯核苷的合成及抗病毒评估。反应方案从受保护的L-苏糖开始,膦酸酯基团通过阿尔布佐夫反应引入。已获得2'-OH以及2'-脱氧核苷。遗憾的是,这些合成化合物均未显示出对HIV和HCV的活性。

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