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    Synthesis of [2.2.1]bicyclo nucleosides
    1.
    发明授权
    Synthesis of [2.2.1]bicyclo nucleosides 有权
    [2.2.1]双环核苷的合成

    公开(公告)号：US06734291B2

    公开(公告)日：2004-05-11

    申请号：US10233177

    申请日：2002-12-16

    申请人： Alexei Kochkine ,  Jef Fensholdt ,  Henrik M. Pfundheller

    发明人： Alexei Kochkine ,  Jef Fensholdt ,  Henrik M. Pfundheller

    IPC分类号： C07H1504

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5′-sulfonated ring-closed intermediate also allows for synthesis of 5′-amino- and thio-LNAs

    摘要翻译： 较短且提供更高总产率的[2.2.1]双环核苷的合成通过通式III的关键中间体进行，其中R 4和R 5为例如磺酸盐，且R 7为例如卤素或 乙酸盐。 从通式II的化合物，如3-O-芳基-4-C-羟甲基-1,2-邻 - 异丙叉-α-D-呋喃核糖，通式Ⅲ的中间体适用于与甲硅烷基化的核碱基偶联。 在形成的[2.2.1]双环核苷上进行一锅碱诱导的闭环和脱磺化，证明了向腺苷，胞嘧啶，尿苷，胸苷和胍的每个LNA（锁定核酸）衍生物的短路径。 使用5'-磺化的闭环中间体还可以合成5'-氨基和硫代-LNA

    Synthesis of [2.2.1]bicyclo nucleosides
    3.
    发明授权
    Synthesis of [2.2.1]bicyclo nucleosides 有权
    [2.2.1]双环核苷的合成

    公开(公告)号：US06639059B1

    公开(公告)日：2003-10-28

    申请号：US09534769

    申请日：2000-03-24

    申请人： Alexei Kochkine ,  Jef Fensholdt ,  Henrik M. Pfundheller

    发明人： Alexei Kochkine ,  Jef Fensholdt ,  Henrik M. Pfundheller

    IPC分类号： C07H1500

    CPC分类号： C07H19/06 ,  C07H19/16

    摘要： A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-&agr;-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5′-sulfonated ring-closed intermediate also allows for synthesis of 5′-amino- and thio-LNAs.

    摘要翻译： 较短且提供更高总产率的[2.2.1]双环核苷的合成通过通式III的关键中间体进行，其中R 4和R 5为例如磺酸盐，且R 7为例如卤素或 乙酸盐。 从通式II的化合物，如3-O-芳基-4-C-羟甲基-1,2-邻 - 异丙叉-α-D-呋喃核糖，通式Ⅲ的中间体适用于与甲硅烷基化的核碱基偶联。 在形成的[2.2.1]双环核苷上进行一锅碱诱导的闭环和脱磺化，证明了向腺苷，胞嘧啶，尿苷，胸苷和胍的每个LNA（锁定核酸）衍生物的短路径。 使用5'-磺化的闭环中间体还可以合成5'-氨基和硫代-LNA。

    Synthesis of stable quinone and photoreactive ketone phosphoramidite reagents for solid phase synthesis of photoreactive-oligomer conjugates
    6.
    发明授权
    Synthesis of stable quinone and photoreactive ketone phosphoramidite reagents for solid phase synthesis of photoreactive-oligomer conjugates 有权
    用于固相合成光反应低聚物共轭物的稳定醌和光反应性亚磷酰胺试剂的合成

    公开(公告)号：US06531591B1

    公开(公告)日：2003-03-11

    申请号：US09611833

    申请日：2000-07-07

    申请人： Jef Fensholdt

    发明人： Jef Fensholdt

    IPC分类号： C07H2100

    CPC分类号： C07H21/00 ,  C07F9/2408

    摘要： Quinone phosphoramidite reagents as well as photoreactive ketone phosphoramidite reagents, such as anthraquinone phosphoramidite reagents and benzophenone phosphoramidite reagents were synthesized and used for the solid phase synthesis of photoreactive-oligonucleotide conjugates. These phosphoramidite reagents are stable, suitable for large-scale synthesis and designed for automated solid phase synthesis of oligomers terminating in a photoreactive moiety.

    摘要翻译： 喹诺酮亚磷酰胺试剂和光反应性亚磷酰胺试剂如蒽醌亚磷酰胺试剂和二苯甲酮亚磷酰胺试剂合成并用于光活化寡核苷酸共轭物的固相合成。 这些亚磷酰胺试剂是稳定的，适用于大规模合成并设计用于自由基固相合成终端于光反应性部分的低聚物。