Labelled oligonucleotides synthesized on solid-supports
    1.
    发明申请
    Labelled oligonucleotides synthesized on solid-supports 有权
    在固体支持物上合成标记的寡核苷酸

    公开(公告)号:US20010014735A1

    公开(公告)日:2001-08-16

    申请号:US09813378

    申请日:2001-03-20

    摘要: Methods and compositions to label oligonucleotides and analogs directly on a solid-support having the structure 1 where S is a solid-support, A is a cleavable linker, X is a moiety with three or more attachment sites, L is a label, Y is a nucleophile, i.e. O, NH, NR or S, and P1 is an acid cleavable protecting group are provided. The labelled solid-support is reacted in a cyclical fashion to synthesize a labelled oligonucleotide on a solid-support in the 5null to 3null direction, having the structure: 2 Labelled oligonucleotides are also synthesized by reacting: (i) a label reagent bearing functionality consisting of carboxylic acid, sulfonic acid, phosphonic acid, or phosphoric acid, (ii) an oligonucleotide on solid support with nucleophilic functionality, and (iii) a coupling reagent, whereby an ester, amide, thioester, sulfonamide, sulfonate, phosphonate, phosphoramidate, phosphorothioate, or phosphate bond is formed. The labelling reaction may be conducted at label sites including the 5null terminus, the 3null terminus, a nucleobase, an internucleotide linkage, a sugar, amino, sulfide, hydroxyl, and carboxyl.

    摘要翻译: 方法和组合物直接在具有S是固体支持物的结构的固体支持物上标记寡核苷酸和类似物,A是可切割的连接体,X是具有三个或更多个连接位点的部分,L是标记,Y是一个 亲核试剂,即O,NH,NR或S,P1是可酸切割的保护基团。 标记的固体支持物以循环方式反应以在5'至3'方向的固体支持物上合成标记的寡核苷酸,具有以下结构:标记的寡核苷酸还通过以下方式合成:(i)标记试剂载体官能团 包括羧酸,磺酸,膦酸或磷酸,(ii)具有亲核官能团的固体支持物上的寡核苷酸,和(iii)偶联剂,其中酯,酰胺,硫酯,磺酰胺,磺酸酯,膦酸酯,氨基磷酸酯 ,硫代磷酸酯或磷酸酯键。 标记反应可以在包括5'末端,3'末端,核碱基,核苷酸间键,糖,氨基,硫化物,羟基和羧基的标记位点进行。

    Multiple-labelled oligonucleotides synthesized on solid-supports
    2.
    发明申请
    Multiple-labelled oligonucleotides synthesized on solid-supports 有权
    在固体支持物上合成多重标记的寡核苷酸

    公开(公告)号:US20020165389A1

    公开(公告)日:2002-11-07

    申请号:US10010717

    申请日:2001-11-07

    IPC分类号: C07H021/04

    摘要: Methods and compositions to label oligonucleotides and analogs directly on a solid-support having the structure 1 where S is a solid-support, A is a cleavable linker, X is a moiety with three or more attachment sites, L is a label, Y is a nucleophile, i.e. O, NH, NR or S, and P1 is an acid cleavable protecting group are provided. The labelled solid-support is reacted in a cyclical fashion to synthesize a labelled oligonucleotide on a solid-support in the 5null to 3null direction, having the structure: 2 Labelled oligonucleotides are also synthesized by reacting: (i) a label reagent bearing functionality consisting of carboxylic acid, sulfonic acid, phosphonic acid, or phosphoric acid, (ii) an oligonucleotide on solid support with nucleophilic functionality, and (iii) a coupling reagent, whereby an ester, amide, thioester, sulfonamide, sulfonate, phosphonate, phosphoramidate, phosphorothioate, or phosphate bond is formed. The labelling reaction may be conducted at label sites including the 5null terminus, the 3null terminus, a nucleobase, an internucleotide linkage, a sugar, amino, sulfide, hydroxyl, and carboxyl.

    摘要翻译: 方法和组合物直接在具有S是固体支持物的结构的固体支持物上标记寡核苷酸和类似物,A是可切割的连接体,X是具有三个或更多个连接位点的部分,L是标记,Y是一个 亲核试剂,即O,NH,NR或S,P1是可酸切割的保护基团。 标记的固体支持物以循环方式反应以在5'至3'方向的固体支持物上合成标记的寡核苷酸,具有以下结构:标记的寡核苷酸还通过以下方式合成:(i)标记试剂载体官能团 包括羧酸,磺酸,膦酸或磷酸,(ii)具有亲核官能团的固体支持物上的寡核苷酸,和(iii)偶联试剂,其中酯,酰胺,硫酯,磺酰胺,磺酸酯,膦酸酯,氨基磷酸酯 ,硫代磷酸酯或磷酸酯键。 标记反应可以在包括5'末端,3'末端,核碱基,核苷酸间键,糖,氨基,硫化物,羟基和羧基的标记位点进行。