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    Process for preparing phosphorothioate oligonucleotides
    2.
    发明授权
    Process for preparing phosphorothioate oligonucleotides 失效
    制备硫代磷酸酯寡核苷酸的方法

    公开(公告)号：US5644048A

    公开(公告)日：1997-07-01

    申请号：US993115

    申请日：1992-12-18

    申请人： Eric K. Yau

    发明人： Eric K. Yau

    IPC分类号： C07H19/04 ,  C07H21/00

    CPC分类号： C07H21/00 ,  C07H19/04

    摘要： A process for preparing phosphorothioate oligonucleotides utilizes S-(alkaryl or aryl) phosphorothioate compounds as intermediates suitable for use in the solution phase. A dinucleotide is prepared from a nucleoside intermediate that has been phosphitylated with an S-(alkaryl or aryl) alkyl phosphorothioate diester salt. The alkyl ester group is removed and the resulting nucleotide diester is reacted with a further nucleoside having a free 5'-hydroxyl group. Nucleotide units are linked together to yield compounds of the structure: ##STR1## where X is H, a first blocking group, a nucleoside, a nucleotide or an oligonucleotide; Y is H, a second blocking group, a nucleoside, a nucleotide or an oligonucleotide; R is an alkaryl or aryl group; n is an integer greater than 0; and Bx is a heterocyclic base. Deblocking of the S-alkaryl or S-aryl moiety yields a phosphorothioate oligonucleotide.

    摘要翻译： 制备硫代磷酸酯寡核苷酸的方法利用S-（烷芳基或芳基）硫代磷酸酯化合物作为适用于溶液相的中间体。 二核苷酸由已经用S-（烷芳基或芳基）烷基硫代磷酸二酯盐磷酸化的核苷中间体制备。 除去烷基酯基团，得到的核苷酸二酯与另外具有游离的5'-羟基的核苷酸反应。 将核苷酸单元连接在一起以产生以下结构的化合物：其中X为H，第一封闭基团，核苷，核苷酸或寡核苷酸; Y为H，第二封闭基团，核苷，核苷酸或寡核苷酸; R是烷芳基或芳基; n是大于0的整数; 而Bx是杂环基。 S-烷芳基或S-芳基部分的去隔离产生硫代磷酸酯寡核苷酸。

    S-(2,4-dichlorobenzyl)-.beta.-cyanoethyl phosphorothioate diester
    3.
    发明授权
    S-(2,4-dichlorobenzyl)-.beta.-cyanoethyl phosphorothioate diester 失效
    S-（2,4-二氯苄基）-β-氰基乙基硫代磷酸二酯

    公开(公告)号：US5210264A

    公开(公告)日：1993-05-11

    申请号：US818928

    申请日：1992-01-10

    申请人： Eric K. Yau

    发明人： Eric K. Yau

    IPC分类号： C07F9/165 ,  C07H19/10 ,  C07H21/00

    CPC分类号： C07H19/10 ,  C07F9/1651 ,  C07F9/1653 ,  C07H21/00

    摘要： The compound S-(2,4-dichlorobenzyl)-.beta.-cyanoethyl phosphorothioate diester is disclosed as useful in the synthesis of phosphorothioate oligonucleotides. In certain embodiments of the invention, this reagent is used to prepare 3'-S-(alkaryl) phosphorothioates. The .beta.-cyanoethyl blocking group can be removed and the resulting diester reacted with a nucleotide having a free 5'-hydroxyl group to yield compounds of the structure: ##STR1## where X is H, a first blocking group, a nucleoside, a nucleotide or an oligonucleotide; Y is H, a second blocking group, a nucleotide or an oligonucleotide; R is an alkaryl or aryl group; n is an integer greater than 0; and Bx is a heterocyclic base. Deblocking of the S-alkaryl or S-aryl moiety yields a phosphorothioate oligonucleotide.

    摘要翻译： 公开了用于合成硫代磷酸酯寡核苷酸的化合物S-（2,4-二氯苄基）-β-氰基乙基硫代磷酸二酯。 在本发明的某些实施方案中，该试剂用于制备3'-S-（烷芳基）硫代磷酸酯。 可以除去β-氰基乙基封闭基团，所得的二酯与具有游离的5'-羟基的核苷酸反应，得到以下结构的化合物：其中X是H，第一个封闭基团，核苷，核苷酸 或寡核苷酸; Y为H，第二封闭基团，核苷酸或寡核苷酸; R是烷芳基或芳基; n是大于0的整数; 而Bx是杂环基。 S-烷芳基或S-芳基部分的去隔离产生硫代磷酸酯寡核苷酸。