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    • 5. 发明授权
    • Reagents for oligonucleotide cleavage and deprotection
    • 寡核苷酸切割和去保护的试剂
    • US06664388B2
    • 2003-12-16
    • US10091231
    • 2002-03-04
    • Jeffrey S. Nelson
    • Jeffrey S. Nelson
    • C07H2104
    • C07H21/00C07H21/04Y02P20/55
    • The present invention provides a process for the removal of protecting groups, i.e. deprotection, from chemically synthesized oligonucleotides. In one embodiment, the invention provides reagents suitable for use in such a process, and kits incorporating such reagents in a convenient, ready-to-use format. By use of the process and reagents of the invention, side-reactions leading to certain impurities that contaminate the synthesized oligonucleotides can be minimized. Methods and reagents are provided for deprotection of an oligonucleotide by reacting a protected oligonucleotide with a deprotection reagent wherein the deprotection reagent comprises an active methylene compound and an amine reagent. The active methylene compound has the structure: where substituent EWG is an electron-withdrawing group and R is hydrogen, C1-C12 alkyl, C6-C20 aryl, heterocycle or an electron-withdrawing group.
    • 本发明提供了从化学合成的寡核苷酸中除去保护基团即脱保护的方法。 在一个实施方案中,本发明提供了适用于这种方法的试剂,以及以便于使用的方式并入这些试剂的试剂盒。 通过使用本发明的方法和试剂,可以使导致某些杂质污染合成的寡核苷酸的副反应最小化。通过使被保护的寡核苷酸与脱保护试剂反应来提供寡核苷酸脱保护的方法和试剂,其中脱保护试剂 包括活性亚甲基化合物和胺试剂。 活性亚甲基化合物具有以下结构:其中取代基EWG为吸电子基团,R为氢,C1-C12烷基,C6-C20芳基,杂环或吸电子基团。