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    • 7. 发明授权
    • Nucleoside-3'-phosphites for synthesis of oligonucleotides
    • 用于合成寡核苷酸的核苷-3'-磷酸酶
    • US5134228A
    • 1992-07-28
    • US412990
    • 1989-09-26
    • Hiroshi Takaku
    • Hiroshi Takaku
    • C07F9/141C07H19/10C07H19/20
    • C07H19/10C07F9/1411C07H19/20Y02P20/55
    • The invention provides novel phosphites represented by the general formula (I) and nucleoside-3'-phosphite derivatives represented by the general formula (III).(RO).sub.3 P (I)wherein R is, for example, a fluoroalkyl group or a substituted phenyl group. ##STR1## wherein R is the same as in (I), R" is a protecting group such as dimethoxytrityl group, and B represents a base, e.g. thymine.A phosphite (I) is prepared by reacting an alcohol ROH with PCl.sub.3 in the presence of a tertiary amine, and a nucleoside-3'-phosphite (III) is prepared by reacting a phosphite (I) with a nucleoside in a solvent in the presence of a tertiary amine. Phosphites (I) are very stable. Using a nucleoside-3'-phosphite (III) an oligonucleotide can be synthesized on a solid support by a simplified process.
    • 本发明提供由通式(I)表示的新型亚磷酸酯和由通式(III)表示的核苷-3'-亚磷酸酯衍生物。 (RO)3P(I)其中R是例如氟代烷基或取代的苯基。 (III)其中R与(I)中的相同,R“是保护基,例如二甲氧基三苯甲基,B表示碱。 胸腺嘧啶 通过在叔胺存在下使醇ROH与PCl 3反应制备亚磷酸酯(I),通过使亚磷酸酯(I)与核苷在溶剂中反应制备核苷-3'-亚磷酸酯(III) 存在叔胺。 亚磷酸酯(I)非常稳定。 使用核苷-3'-亚磷酸酯(III),可以通过简化的方法在固体支持物上合成寡核苷酸。