Abstract A simple and convenient synthetic protocols based on H-phosphonate chemistry have been developed for the preparation of nucleoside 5′-diphosphates. It consists of oxidation of the silylated H-phosphonate monoesters in pyridine with iodine to produce the corresponding N-pyridiniumphosphonate intermediates, followed by their reactions with orthophosphoric acid used as a nucleophile. The added value of the method is that substrates for the reaction, H-phosphonate monoesters, can be prepared in situ from the corresponding nucleosides and used for the next step without isolation. The procedure is simple and applicable to the preparation of various diphosphates of ribo- and deoxyribonucleosides, and their analogues. Graphical Abstract

中文翻译：

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从核苷 5'-H-膦酸酯单酯实际合成核苷 5'-二磷酸

摘要 已经开发了一种基于 H-膦酸酯化学的简单方便的合成方案，用于制备核苷 5'-二磷酸。它包括在吡啶中用碘氧化甲硅烷基化的 H-膦酸酯单酯以产生相应的 N-吡啶鎓膦酸酯中间体，然后它们与用作亲核试剂的正磷酸反应。该方法的附加值是反应的底物 H-膦酸酯单酯可以由相应的核苷原位制备，无需分离即可用于下一步。该方法简单，适用于核糖和脱氧核糖核苷的各种二磷酸盐及其类似物的制备。图形概要