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    Cephalosporin sulfoxides
    32.
    发明授权
    Cephalosporin sulfoxides 失效
    CEPHALOSPORIN SULFOXIDES

    公开(公告)号：US3597421A

    公开(公告)日：1971-08-03

    申请号：US3597421D

    申请日：1969-01-21

    申请人： LILLY CO ELI

    发明人： WEBBER J ALLAN

    IPC分类号： C07D501/04 ,  C07D501/24 ,  C07D99/24

    CPC分类号： C07D501/04

    摘要： A NUMBER OF NOVEL 3-FUNCTIONALIZEDMETHYL CEPHALOSPORIN SULFOXIDES WHICH ARE USEFUL INTERMEDIATES IN THE PREPARATION OF CEPHALOSPORIN ANTIBIOTICS ARE DISCLOSED AND CLAIMED. THESE NOVEL SULFOXIDES ARE OBTAINED BY THE OXIDATION OF THE CORRESPONDING CEPHALOSPORIN COMPOUNDS.

    CEPHALOSPORIN COMPOUND
    36.
    发明申请
    CEPHALOSPORIN COMPOUND 审中-公开
    CEPHALOSPORIN化合物

    公开(公告)号：US20150025053A1

    公开(公告)日：2015-01-22

    申请号：US14333966

    申请日：2014-07-17

    申请人： Cubist Pharmaceuticals, Inc.

    发明人： Yong He ,  Yu Gui Gu ,  Ning Yin

    IPC分类号： C07D501/60 ,  C07D501/04

    CPC分类号： C07D501/60 ,  C07D501/04 ,  C07D501/56

    摘要： The cephalosporin compound of formula (I) is disclosed, which exhibits antibiotic activity against Gram-negative (e.g., Pseudomonas aeruginosa) and Gram-positive (e.g., methicillin-resistant Staphylococcus aureus) bacteria. Methods of manufacturing the compound of formula (I), and uses of the compound in the preparation of pharmaceutical compositions and antibacterial applications are also disclosed.

    摘要翻译： 公开了式（I）的头孢菌素化合物，其表现出抗革兰氏阴性（例如铜绿假单胞菌）和革兰氏阳性（例如耐甲氧西林金黄色葡萄球菌）细菌的抗生素活性。 还公开了制备式（I）化合物的方法，以及该化合物在制备药物组合物和抗菌应用中的用途。

    Process for the preparation of cefditoren
    40.
    发明申请
    Process for the preparation of cefditoren 失效
    头孢托仑的制备方法

    公开(公告)号：US20060173175A1

    公开(公告)日：2006-08-03

    申请号：US10563371

    申请日：2004-07-03

    申请人： Kumar Prabhat ,  Anandam Vempali ,  Sivakumaran Sundaravadivelan ,  Nagesh Praveen ,  Manikrao Vittal ,  Balawant Pandurang ,  Kumar Parven ,  Ramesh Pratik

    发明人： Kumar Prabhat ,  Anandam Vempali ,  Sivakumaran Sundaravadivelan ,  Nagesh Praveen ,  Manikrao Vittal ,  Balawant Pandurang ,  Kumar Parven ,  Ramesh Pratik

    IPC分类号： C07D501/14

    CPC分类号： C07D501/04

    摘要： The present invention relates to an improved process for the preparation of Cefditoren of formula (I), the said process comprising the steps of: i) converting the compound of formula (II) to a compound of the formula (III) using TPP and sodium iodide in the presence of THF, water, and base; ii) reacting the compound of formula (III) with 4-methyl-5-formyl-thiazole to produce a compound of formula (IV); iii) deesterifying the compound of the formula (IV) to yield compound of formula (V); iv) converting the compound of formula (V) to compound of formula (VI) in the presence of a base and solvent; v) converting the compound of formula (VI) into compound of formula (VII) by enzymatic hydrolysis; and vi) reacting compound of formula (VII) with compound of formula (VIII) in the presence of solvent and base to produce compound of formula (I).

    摘要翻译： 本发明涉及制备式（I）的头孢托仑的改进方法，所述方法包括以下步骤：i）使用TPP和钠将式（II）化合物转化为式（III）化合物 碘化物在THF，水和碱的存在下反应; ii）使式（III）化合物与4-甲基-5-甲酰基 - 噻唑反应以制备式（IV）化合物; iii）将式（Ⅳ）化合物酯化，得到式（Ⅴ）化合物; iv）在碱和溶剂的存在下将式（Ⅴ）化合物转化成式（Ⅵ）化合物; v）通过酶水解将式（Ⅵ）化合物转化成式（Ⅶ）化合物; 和vi）使式（VII）的化合物与式（VIII）的化合物在溶剂和碱的存在下反应，得到式（I）的化合物。