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    MULTIPLE COUPLING & OXIDATION METHOD
    5.
    发明申请
    MULTIPLE COUPLING & OXIDATION METHOD 审中-公开

    公开(公告)号：US20200148714A1

    公开(公告)日：2020-05-14

    申请号：US16617279

    申请日：2018-06-26

    申请人： Roche Innovation Center Copenhagen A/S

    发明人： Dennis Jul Hansen ,  Erik Daa Funder

    IPC分类号： C07H1/00 ,  C07H21/00

    摘要： The present invention relates to the field of stereodefined phosphorothioate oligonucleotides and to stereodefining nucleoside monomers and methods of synthesis of stereodefined oligonucleotides using said monomer. Herein are disclosed oligonucleotide enhanced synthesis methods where within a single elongation cycle there are repeated coupling and oxidation steps. The method results in an enhanced yield and higher purity of stereodefined phosphorothioate oligonucleotides

    Multiple coupling and oxidation method
    6.
    发明授权
    Multiple coupling and oxidation method 有权

    公开(公告)号：US11814407B2

    公开(公告)日：2023-11-14

    申请号：US16617279

    申请日：2018-06-26

    申请人： Roche Innovation Center Copenhagen A/S

    发明人： Dennis Jul Hansen ,  Erik Daa Funder

    IPC分类号： C07H21/00 ,  C07H21/02 ,  C07H21/04 ,  C07H1/00

    CPC分类号： C07H1/00 ,  C07H21/00 ,  C07H21/02 ,  C07H21/04

    摘要： The present invention relates to methods of synthesis of stereodefined oligonucleotides wherein the protected 5′-hydroxy terminus of a nucleoside or oligonucleotide attached to a solid support is first unprotected, followed by coupling an oxazaphospholidine phosphoramidite monomer to the now deprotected 5′-hydroxy terminus, oxidizing the resultant phosphite triester intermediate with a sulfurizing reagent, and optionally washing the product. The method of synthesis of the present invention described above may be repeated to optionally elongate the stereodefined oligonucleotide being synthesized until the elongation cycle is intentionally terminated via deprotecting and cleavaging the resulting stereodefined oligonucleotide from the solid support. The oxazaphospholidine phosphoramidite monomer to be coupled in the present invention may optionally be chosen from Formula 1a and 1b. Generally, the present invention relates to enhanced synthesis methods wherein a single elongation cycle, optionally comprising repeated coupling and oxidation steps, results in an enhanced yield and higher purity of stereodefined phosphorothioate oligonucleotides.

    Stereodefining L-monomers
    9.
    发明授权
    Stereodefining L-monomers 有权

    公开(公告)号：US11267843B2

    公开(公告)日：2022-03-08

    申请号：US16086252

    申请日：2017-03-02

    申请人： Roche Innovation Center Copenhagen A/S

    发明人： Nanna Albaek ,  Jacob Ravn ,  Erik Daa Funder

    IPC分类号： C07H19/16

    摘要： Stereodefined phosphorothioate oligonucleotides, related nucleoside monomers and methods of synthesis of both are described. The disclosed isobutyryl protected L-LNA-G monomers have following Formula 50 or 51 where R3 is independently CH2ODMTr or CH2OMMTr and R8, when present, is cyanoethyl. The monomers have improved solubility and stability characteristics, resulting in improved efficacy in oligonucleotide synthesis.