发明名称 Process for preparing oligonucleotides having chiral phosphorus linkages
摘要 Sequence-specific oligonucleotides are provided having substantially pure chiral Sp phosphorothioate, chiral Rp phosphorothioate, chiral Sp alkylphosphonate, chiral Rp alkylphosphonate, chiral Sp phosphoamidate, chiral Rp phosphoamidate, chiral Sp phosphotriester, and chiral Rp phosphotriester linkages. The novel oligonucleotides are prepared via a stereospecific SN2 nucleophilic attack of a phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate anion on the 3' position of a xylonucleotide. The reaction proceeds via inversion at the 3' position of the xylo reactant species, resulting in the incorporation of phosphodiester, phosphorothioate, phosphoramidate, phosphotriester or alkylphosphonate linked ribofuranosyl sugar moieties into the oligonucleotide.
申请公布号 US5521302(A) 申请公布日期 1996.05.28
申请号 US19930058023 申请日期 1993.05.05
申请人 ISIS PHARMACEUTICALS, INC. 发明人 COOK, PHILLIP D.
分类号 A61K38/00;A61K48/00;C07H19/04;C07H19/06;C07H19/10;C07H19/16;C07H19/20;C07H21/00;C07H23/00;C07J43/00;C12N9/02;C12N15/10;C12N15/113;C12P19/34;C12Q1/68;C12Q1/70;(IPC1-7):C07H1/00;C07H21/04 主分类号 A61K38/00
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