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    • 4. 发明申请
    • RAPID SOLID PHASE SYNTHESIS OF OLIGONUCLEOTIDES USING PHOSPHORUS OXYCHLORIDE ACTIVATION
    • 使用磷酰氯活化的快速固相合成寡核苷酸
    • WO1982003079A1
    • 1982-09-16
    • PCT/US1982000305
    • 1982-03-09
    • BIORESEARCH INC
    • BIORESEARCH INCVERLANDER MICHAEL SFULLER WILLIAM DEANGOODMAN MURRAY
    • C07H21/02
    • C07H21/00
    • A method for the synthesis of oligonucleotides which comprises the steps of packing a flow reactor with supported nucleoside comprised of a first nucleoside attached at its 5'-position of an insoluble solid support, activating said support-nucleoside by treatment with phosphorus oxychloride in the presence of a basic catalyst to provide a 3'-dichlorophosphoryl group on said first nucleoside, coupling a second similar or dissimilar nucleoside, unprotected at the 3'-and 5'-position, to said first nucleoside by condensation with said dichlorophosphoryl group and repeating said activation and coupling step until the desired oligonucleotide sequence is obtained. The oligonucleotide may then be recovered by cleavage from the support and purified, if required.
    • 一种用于合成寡核苷酸的方法,其包括以下步骤:将具有负载的核苷的流动反应器包装,所述核苷包含在其不溶性固体支持物的5'-位上附着的第一核苷,在存在的情况下通过用磷酰氯处理来活化所述载体核苷 的碱性催化剂,以在所述第一核苷上提供3'-二氯磷酰基,通过与所述二氯磷酰基缩合,将在3'和5'-位未被保护的第二相似或不同的核苷与所述第一核苷偶联,并重复所述 活化和偶联步骤,直到获得所需的寡核苷酸序列。 然后,如果需要,可以通过从载体中切割回收寡核苷酸并进行纯化。