Synthesis of 2′,3′— and 3′,5′—cyclic phosphate mono-and oligonucleotides
    3.
    发明授权
    Synthesis of 2′,3′— and 3′,5′—cyclic phosphate mono-and oligonucleotides 有权
    2',3'和3',5'-环磷酸酯单 - 和寡核苷酸的合成

    公开(公告)号:US08618279B2

    公开(公告)日:2013-12-31

    申请号:US12657227

    申请日:2010-01-15

    IPC分类号: C07H19/20

    摘要: The invention provides a novel method for the chemical synthesis of 2′,3′-cyclic phosphate and phosphorothioate of mono and terminated oligonucleotides synthesis. The invention also provides a novel method of for the chemical synthesis of 2′,3′- and 3′,5′-cyclic phosphate and phosphorothioate mononucleotide nucleotides. The process is based on quick and efficient cyclization of phosphoramidate moiety and neighboring hydroxyl group. The present invention is directed towards the synthesis of high purity DNA and RNAs, specifically to introduce cyclic phosphate at 3′-end of oligonucleotides. Such DNA and RNA's have extensive application in therapeutics, diagnostics, drug design, and selective inhibition of an RNA sequence within cellular environment, in pre-tRNA cleavage and in ribozyme ligation. The 2′,3′-cyclic phosphate nucleosides are involved in a vast number of applications in molecular biology in general and mammalian cells in particular. The invention also envisions providing kits comprising at least one composition disclosed in the present invention.

    摘要翻译: 本发明提供了一种用于化学合成单和末端寡核苷酸合成的2',3'-环磷酸酯和硫代磷酸酯的新方法。 本发明还提供了化学合成2',3'和3',5'环磷酸和硫代磷酸酯单核苷酸核苷酸的新方法。 该方法基于氨基磷酸酯部分和相邻羟基的快速有效的环化。 本发明涉及高纯度DNA和RNA的合成,特别是在寡核苷酸的3'-末端引入环状磷酸酯。 这种DNA和RNA在治疗,诊断,药物设计和细胞环境中的RNA序列的选择性抑制,前tRNA切割和核酶连接中都有广泛的应用。 2',3'-环磷酸核苷在一般的分子生物学和特别是哺乳动物细胞中涉及广泛的应用。 本发明还设想提供包含本发明公开的至少一种组合物的试剂盒。