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    • 8. 发明授权
    • Preparation of oligodeoxyribonucleoside alkyl or arylphosphonates
    • 寡脱氧核糖核苷烷基或芳基膦酸酯的制备
    • US4507433A
    • 1985-03-26
    • US540185
    • 1983-10-07
    • Paul S. MillerPaul O. P. Ts'O
    • Paul S. MillerPaul O. P. Ts'O
    • C07H21/00C07H21/02C07H21/04
    • C07H21/00Y02P20/55
    • Process for synthesizing deoxyribonucleoside methylphosphonates on polystyrene polymer supports which involves condensing 5'-dimethoxytrityldeoxynucleoside 3'-methylphosphonates. The oligomers are removed from the support and the base protecting groups hydrolyzed by treatment with ethylenediamene in ethanol, which avoids hydrolysis of the methylphosphonate linkages. Two types of oligomers are synthesized: those containing only methylphosphonate linkages, d-Np(Np).sub.n N, and those which terminate with a 5' nucleotide residue, dNp(Np).sub.n N. The latter oligomers can be phosphorylated by polynucleotide kinase, and are separated by polyacrylamide gel electrophoresis according to their chain length. Piperidine randomly cleaves the oligomer methylphosphonate linkages and generates a series of shorter oligomers whose number corresponds to the length of the original oligomer. Apurinic sites introduced by acid treatment spontaneously hydrolyze to give oligomers which terminate with free 3' and 5'-OH groups. These reactions may be used to characterize the oligomers.
    • 在聚苯乙烯聚合物载体上合成脱氧核糖核苷甲基膦酸酯的方法,其涉及使5'-二甲氧基三脱氧核苷3'-甲基膦酸酯缩合。 从载体中除去低聚物,碱性保护基团通过在乙醇中用乙二胺处理而水解,这避免了甲基膦酸酯键的水解。 合成两种类型的低聚物:仅含甲基膦酸酯键,d-Np(Np)nN和终止于5'核苷酸残基dNp(Np)nN的低聚物。 后者的寡聚体可以被多核苷酸激酶磷酸化,并根据其链长度通过聚丙烯酰胺凝胶电泳分离。 哌啶随机切割低聚物甲基膦酸酯键,并产生一系列较短的低聚物,其数量对应于原始低聚物的长度。 通过酸处理引入的无麸质位点自发水解,得到以游离的3'和5'-OH基团终止的低聚物。 这些反应可用于表征低聚物。