Poecke Sara Van, Sinnaeve Davy, Martins José C, Balzarini Jan, Calenbergh Serge Van
Laboratory for Medicinal Chemistry, Faculty of Pharmaceutical Sciences, Ghent University, Gent, Belgium.
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。
