5-取代的2'-脱氧尿苷-5'-膦酸酯类似物的合成及其抗病毒活性评估。
Synthesis of 5-substituted 2'-deoxyuridine-5'- phosphonate analogues and evaluation of their antiviral activity.
作者信息
Poecke Sara Van, Sinnaeve Davy, Martins José C, Balzarini Jan, Calenbergh Serge Van
机构信息
Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Gent, Belgium.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2012;31(3):256-72. doi: 10.1080/15257770.2012.654876.
A small series of 5-(hetero)aryl-modified nucleoside phosphonates was synthesized via an 8-step procedure including a Wittig reaction and Suzuki-Miyaura coupling. An unanticipated anomerization during phosphonate deprotection allowed us to isolate both anomers of the 5-substituted 2'-deoxy-uridine phosphonates and assess their antiviral activity against a broad panel of viruses.
通过包括维蒂希反应和铃木-宫浦偶联在内的8步程序合成了一小系列5-（杂）芳基修饰的核苷膦酸酯。膦酸酯脱保护过程中意外的异头物异构化使我们能够分离出5-取代的2'-脱氧尿苷膦酸酯的两种异头物，并评估它们对多种病毒的抗病毒活性。
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