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25 条记录 (耗时 0.02 秒)

    Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors
    22.
    发明授权
    Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors 失效
    导致氟化逆转录酶抑制剂制备的关键中间体的非对映选择性过程

    公开(公告)号：US5498719A

    公开(公告)日：1996-03-12

    申请号：US189095

    申请日：1994-01-31

    申请人： Victor E. Marquez ,  John S. Driscoll ,  Magbool A. Siddiqui

    发明人： Victor E. Marquez ,  John S. Driscoll ,  Magbool A. Siddiqui

    IPC分类号： C07D317/26 ,  C07D317/30 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D317/26 ,  C07D317/30

    摘要： The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.

    摘要翻译： 本发明提供了一种关键前体的新型合成途径，即用于制备FddA的（S，S）-α-氟-2,2-二甲基-1,3-二氧戊环-4-丙酸酯 FddC。 即时非对映选择性方法利用含有手性助剂的新型中间体。 手性助剂可以是任何手性辅助部分，例如含有取代的恶唑烷酮基团的助剂。 包含手性助剂的中间体在氟化糖的合成中首次使用氟化方法进行氟化，得到氟化中间体，其在除去手性基团后提供所需的关键中间体。 总之，在本发明的方法中，通过手性烯醇化物与亲电氟化剂的反应将氟非对映选择性引入中间体，并且氟化的中间体衍生自甘露醇。

    Phosphoramidite reagent for chemical synthesis of modified DNA
    24.
    发明授权
    Phosphoramidite reagent for chemical synthesis of modified DNA 失效
    用于化学合成修饰DNA的亚磷酰胺试剂

    公开(公告)号：US5324831A

    公开(公告)日：1994-06-28

    申请号：US178153

    申请日：1988-04-06

    申请人： Victor E. Marquez ,  Amanda J. Goddard

    发明人： Victor E. Marquez ,  Amanda J. Goddard

    IPC分类号： C07H1/02 ,  C07H19/04 ,  C07H19/12 ,  C07H19/23 ,  C07H21/00 ,  C07H21/04 ,  C07H1/00

    CPC分类号： C07H19/04 ,  C07H19/12 ,  C07H21/00

    摘要： 5,6-dihydro-5-azacytidine phosphoramidite is useful in the synthesis of oligonucleotides and DNA containing dihydro-5-aza- and 5-azacytosine bases. The modified oligonucleotides which contain 5-azacytosine residues at specific sites can be used to determine the mechanism of selective gene activation and the relationship existing between the presence of the triazine base and inhibition of DNA methylation.

    摘要翻译： 5,6-二氢-5-氮杂胞嘧啶亚磷酰胺可用于合成含有二氢-5-氮杂和5-氮杂胞嘧啶碱基的寡核苷酸和DNA。 在特定部位含有5-氮胞嘧啶残基的经修饰的寡核苷酸可用于确定选择性基因激活的机制以及三嗪碱的存在与DNA甲基化抑制之间的关系。