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    PNA synthesis using a base-labile amino protecting group
    7.
    发明授权
    PNA synthesis using a base-labile amino protecting group 失效
    使用碱不稳定氨基保护基的PNA合成

    公开(公告)号：US6121418A

    公开(公告)日：2000-09-19

    申请号：US967197

    申请日：1997-10-29

    申请人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    发明人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    IPC分类号： C07C231/02 ,  C07C233/36 ,  C07C233/47 ,  C07C237/12 ,  C07D239/46 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K1/00 ,  C07K1/04 ,  C07K1/113 ,  C07K5/04 ,  C07K14/00 ,  C07K14/485 ,  C07K14/52 ,  C08G69/10

    CPC分类号： C07D239/47 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K14/003 ,  C08G69/10 ,  Y02P20/55

    摘要： PNA synthesis using a base-labile amino protecting group Processes are described for preparing PNA oligomers, ##STR1## in which R.sup.0 is hydrogen, alkanoyl, alkoxycarbonyl, cycloalkanoyl, aroyl, heteroaroyl, or a group which favors the intracellular uptake of the oligomer, A and Q are amino acid residues, k and 1 are 0 to 20, n is 1-50, B is a nucleotide base which is customary in nucleotide chemistry, and Q.sup.0 is OH, NH.sub.2, or alkylamino which can be substituted by OH or NH.sub.2. In these processes, the amino acid residues and the structural components ##STR2## in which PG is a base-labile amino protecting group and B' is a nucleotide base which is protected on its exocyclic amino function, are coupled step-wise, in accordance with the solid-phase method, onto a polymeric support which is provided with an anchor group, and, after the construction is complete, the target compounds are cleaved from the polymeric support using a cleaving reagent. Intermediates of the PNA oligomers are also described, as are processes for their preparation.

    摘要翻译： 描述了使用碱不稳定氨基保护基的PNA合成制备PNA寡聚体的方法，其中R 0是氢，烷酰基，烷氧基羰基，环烷酰基，芳酰基，杂芳酰基或有利于寡聚体的细胞内摄取的基团A和Q是 氨基酸残基k和1为0至20，n为1-50，B为核苷酸化学中常见的核苷酸碱基，Q0为OH，NH2或可被OH或NH2取代的烷基氨基。 在这些方法中，PG是碱不稳定氨基保护基团的氨基酸残基和结构组分，B'是其外环氨基功能受保护的核苷酸碱基，按照固体 在具有锚定基团的聚合物载体上，并且在构建完成后，使用裂解试剂从聚合物载体上切割目标化合物。 还描述了PNA低聚物的中间体，以及它们的制备方法。

    Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids
    9.
    发明授权
    Substituted N-ethylglycine derivatives for preparing PNA and PNA/DNA hybrids 有权
    用于制备PNA和PNA / DNA杂交体的取代的N-乙基甘氨酸衍生物

    公开(公告)号：US06465650B1

    公开(公告)日：2002-10-15

    申请号：US09506901

    申请日：2000-02-18

    申请人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    发明人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    IPC分类号： C07D47316

    CPC分类号： C07D233/92 ,  C07D231/12 ,  C07D233/56 ,  C07D239/47 ,  C07D239/54 ,  C07D249/08 ,  C07D473/18 ,  C07D473/34 ,  Y02P20/55

    摘要： The invention provides a processes for the preparation of a compound of Formula I, or a salt thereof wherein PG is a urethane- or trityl-type protective group; X is NH, O, or S; Y is CH2, O, or NH; and B′ is a base customary in nucleotide chemistry. The processes include reacting a compound of Formula (II) with a compound of Formula (III) a compound of Formula (V) B′—CH2—CO—R2  (V), a monohaloacetic acid derivative in a suitable solvent with an auxiliary base, or a compound of Formula (VII) B′—CH2—CO—R3  (VII), and converting the resulting compounds to that of Formula I.

    摘要翻译： 本发明提供制备式I化合物或其盐的方法，其中PG是氨基甲酸酯或三苯甲基型保护基; X是NH，O或S; Y是CH 2，O或NH; 而B'是核苷酸化学中常见的基础。 所述方法包括使式（II）化合物与式（III）化合物与式（Ⅴ）化合物在合适的溶剂中与辅助碱或式（Ⅶ）化合物反应，将式（Ⅴ）化合物与单卤代乙酸衍生物反应， 得到的化合物为式I化合物。

    PNA synthesis using a base-labile amino protecting group
    10.
    发明授权
    PNA synthesis using a base-labile amino protecting group 有权
    使用碱不稳定氨基保护基的PNA合成

    公开(公告)号：US06316595B1

    公开(公告)日：2001-11-13

    申请号：US09495457

    申请日：2000-02-01

    申请人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    发明人： Gerhard Breipohl ,  Eugen Uhlmann ,  Jochen Knolle

    IPC分类号： C07K100

    CPC分类号： C07D239/47 ,  C07D239/54 ,  C07D473/18 ,  C07D473/34 ,  C07K14/003 ,  C08G69/10 ,  Y02P20/55

    摘要： The invention provides compounds and processes for synthesis of peptide nucleic acids (PNA). The compounds include temporary amino protecting groups that are base-labile, and protection groups for the exocyclic amino function of the nucleotide base that is compatible with the base-labile amino protecting group. Cleavage of an oligomer comprising these compounds from a solid support can be achieved using weak or medium strength acids.

    摘要翻译： 本发明提供了用于合成肽核酸（PNA）的化合物和方法。 这些化合物包括碱基不稳定的临时氨基保护基，和与碱不稳定氨基保护基相容的核苷酸碱基的环外氨基官能团的保护基。 包含这些化合物的低聚物从固体支持物的切割可以使用弱或中等强度的酸来实现。