新型环戊烯膦酸核苷的简便合成及其抗HIV活性
Simple synthesis and anti-HIV activity of novel cyclopentene phosphonate nucleosides.
作者信息
Kim Aihong, Hong Joon Hee
机构信息
College of Pharmacy, Chosun University, Kwangju, Republic of Korea.
出版信息
Nucleosides Nucleotides Nucleic Acids. 2006;25(1):1-8. doi: 10.1080/15257770500377698.
A very simple synthetic route for novel cyclopentene phosphonate nucleosides is described. The characteristic cyclopentene moiety 6 was constructed via a ring-closing metathesis of divinyl 5, which could be readily prepared from diethylmalonate. The condensation of the mesylate 11 with nucleobases (A, C, T, U) under nucleophilic substitution conditions (K2CO3, 18-Crown-6, DMF) afforded the target nucleosides 12, 13, 14, and 15. In addition, the antiviral evaluations against various viruses were performed.
描述了一种用于新型环戊烯膦酸核苷的非常简单的合成路线。通过二乙烯基 5 的闭环复分解反应构建了特征性的环戊烯部分 6，二乙烯基 5 可由丙二酸二乙酯轻松制备。在亲核取代条件下（碳酸钾、18-冠醚-6、N,N-二甲基甲酰胺），甲磺酸酯 11 与核苷碱（腺嘌呤、胞嘧啶、胸腺嘧啶、尿嘧啶）缩合得到目标核苷 12、13、14 和 15。此外，还对各种病毒进行了抗病毒评估。
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