Large-scale synthesis of a key catalytic reagent for phosphorus protection in building blocks for isopolar phosphonate oligonucleotide preparation

D Rejman, J Erbs, I Rosenberg

文献索引：Rejman, Dominik; Erbs, Jiri; Rosenberg, Ivan Organic Process Research and Development, 2000 , vol. 4, # 6 p. 473 - 476

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被引用次数: 5

摘要

A simple procedure for the large-scale synthesis of 4-methoxy-2-pyridinemethanol 1-oxide (5), a key compound in modern triester synthesis of oligonucleotides, employing Büchi R 152 evaporator as a reaction apparatus was elaborated. Two crucial reaction steps, both strongly exothermic, were satisfactorily handled. Our procedure provides a high-purity, light- and heat-stable product in a satisfactory yield.