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    • 11. 发明申请
    • Activator bound solid supports for nucleic acid synthesis via the phosphoramidite approach
    • 活化剂通过亚磷酰胺方法结合核酸合成的固体支持物
    • US20070135626A1
    • 2007-06-14
    • US11301020
    • 2005-12-12
    • Nam NgoLaurent Jaquinod
    • Nam NgoLaurent Jaquinod
    • C07H21/00C08G63/91
    • C07H21/00
    • The present invention relates to improved methods for the preparation of nucleic acids. More particularly, conventional solid supports used for nucleic acid synthesis are derivatized with activators having pKas within the 4 to 7 range. Preferentially, CPG-based solid supports are reacted with trialkoxysilanes containing an activator moiety such as pyridine. During each deblocking step of the nucleic acid synthesis cycle, bound pyridiniums are generated, yielding a weak acidic medium spreads throughout the solid support. The bound activators efficiently activate the phosphoramidite reagents towards coupling with 5′-hydroxynucleosides bound to the solid supports, thus eliminating or supplementing external deliveries of activator during the coupling steps.
    • 本发明涉及用于制备核酸的改进方法。 更具体地,用于核酸合成的常规固体支持物用具有4至7范围内的pKas的激活剂衍生化。 优选地,将基于CPG的固体载体与含有活化剂部分如吡啶的三烷氧基硅烷反应。 在核酸合成循环的每个去封闭步骤期间,产生结合的吡啶鎓,产生弱酸性介质遍及整个固体支持物。 结合的活化剂有效地活化亚磷酰胺试剂以与与固体支持物结合的5'-羟基核苷偶联,从而在偶联步骤期间消除或补充活化剂的外部输送。