利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

8 条记录 (耗时 0.019 秒)

    Intermediates for providing functional groups on the 5' end of oligonucleotides
    6.
    发明授权
    Intermediates for providing functional groups on the 5' end of oligonucleotides 失效
    用于在寡核苷酸的5'末端提供官能团的中间体

    公开(公告)号：US5391785A

    公开(公告)日：1995-02-21

    申请号：US915589

    申请日：1992-07-15

    申请人： David S. Jones ,  John P. Hachmann ,  Michael J. Conrad ,  Stephen Coutts ,  Douglas A. Livingston

    发明人： David S. Jones ,  John P. Hachmann ,  Michael J. Conrad ,  Stephen Coutts ,  Douglas A. Livingston

    IPC分类号： A61K39/35 ,  A61K47/48 ,  C07C323/12 ,  C07D317/20 ,  C07F9/24 ,  C07F9/655 ,  C07H21/00 ,  C07B39/00

    CPC分类号： C07H21/00 ,  A61K39/35 ,  A61K47/48315 ,  C07C323/12 ,  C07D317/20 ,  C07F9/2408 ,  C07F9/65515 ,  A61K2039/6093 ,  Y02P20/55

    摘要： Phosphoramidites of the formula ##STR1## where R is a base-labile protecting group, R.sup.1 and R.sup.2 are individually alkyl of 1 to 6 carbon atoms, cycloalkyl of 3 to 8 carbon atoms, or aryl of 6 to 20 carbon atoms or are joined together to form with the nitrogen atom a cyclic structure of 4-7 carbon atoms and 0 to 1 annular chalcogen atoms of atomic number 8 to 16, G is a hydrocarbylene group of 1 to 20 carbon atoms and Z is a hydroxy-protected vicinal diol group bound to G by one of the vicinal diol carbon atoms or a disulfide group and bound to G by one of the sulfur atoms of the disulfide group, with the proviso that G is of at least 4 carbon atoms when Z is said disulfide group are used in conventional automated oligonucleotide synthesis to introduce a functional aldehyde or thiol group on the 5' end of the oligonucleotide to thereby provide a reactive site on the oligonucleotide that may be used to conjugate the oligonucleotide to molecules that contain a free amino group or an electrophilic center reactive with a thiol group.

    摘要翻译： 其中R为碱不稳定保护基的式（ⅩⅥ）的亚磷酰胺，R 1和R 2分别为1至6个碳原子的烷基，3至8个碳原子的环烷基或6至20个碳原子的芳基或连接在一起 与氮原子一起形成原子数为8〜16的4-7个碳原子和0〜1个环状硫族原子的环状结构，G为碳原子数1〜20的亚烃基，Z为羟基保护的邻二醇基 通过邻位二醇碳原子之一或二硫键与G结合，并且通过二硫基的硫原子之一与G结合，条件是当Z为所述二硫基时，G为至少4个碳原子 在常规的自动化寡核苷酸合成中，在寡核苷酸的5'末端引入功能性醛或硫醇基团，从而在寡核苷酸上提供可用于将寡核苷酸与含有游离氨基或电离子的分子缀合的反应性位点 与硫醇基反应的中间体。