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    Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
    2.
    发明授权
    Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds 失效
    噻唑乙酸的硫酯衍生物及其在制备头孢菌素化合物中的用途

    公开(公告)号：US06610845B1

    公开(公告)日：2003-08-26

    申请号：US10035177

    申请日：2002-01-04

    申请人： Pandurang Balwant Deshpande ,  Pramod Narayan Deshpande ,  Shanmugam Srinivasan ,  Parven Kumar Luthra ,  Gautam Kumar Das

    发明人： Pandurang Balwant Deshpande ,  Pramod Narayan Deshpande ,  Shanmugam Srinivasan ,  Parven Kumar Luthra ,  Gautam Kumar Das

    IPC分类号： C07D50136

    CPC分类号： C07D417/12 ,  C07D501/00

    摘要： The present invention provides new thioester derivatives of thiazolyl acetic acid of the general formula (I), wherein, R1 represents H, trityl, CH3, CRaRbCOOR2 (Ra and Rb independently of one another represents hydrogen or methyl and R2 represents H or C1-C4 alkyl). also, the invention provides a method by which the said thioester derivatives can be prepared by reacting thiazolyl acetic acid of the general formula (IV) with 1,2,5,6 tetrahdro-2-methyl-5,6 dioxo-1,2,4-triazin-3-thiol of the formula (VI) in a solvent, in presence of an organic base and with the help of Vilsmeier reagent of the formula (V). The so obtained thioester derivatives are reacted with 7-amino-cephem carboxylic acids of the general formula (III) to produce cephalosporin antibiotic compounds having the general formula (II).

    摘要翻译： 本发明提供了通式（I）的噻唑基乙酸的新型硫代酯衍生物，其中R1表示H，三苯甲基，CH3，CRaRbCOOR2（Ra和Rb彼此独立地表示氢或甲基，R2表示H或C1-C4 烷基），本发明提供了一种通过使通式（IV）的噻唑基乙酸与1,2,5,6四氢-2-甲基-5,6-二氧代 - （VI）的1,2,4-三嗪-3-硫醇在有机碱的存在下和借助于式（Ⅴ）的维尔斯迈尔试剂的溶液中进行。 将如此得到的硫酯衍生物与通式（III）的7-氨基头孢烯羧酸反应，生成具有通式（II）的头孢菌素抗生素化合物。