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    Process for the preparation of cefditoren
    2.
    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。

    Method for the preparation of ceftiofur sodium and its intermediates
    3.
    发明授权
    Method for the preparation of ceftiofur sodium and its intermediates 失效
    头孢噻呋钠及其中间体的制备方法

    公开(公告)号：US06800756B2

    公开(公告)日：2004-10-05

    申请号：US10207103

    申请日：2002-07-30

    申请人： Pandurang Balwant Deshpande ,  Praven Kumar Luthra ,  Pratik Ramesh Sathe ,  Sivakumaran Sundaravadivelan ,  Praveen Nagesh Ganesh

    发明人： Pandurang Balwant Deshpande ,  Praven Kumar Luthra ,  Pratik Ramesh Sathe ,  Sivakumaran Sundaravadivelan ,  Praveen Nagesh Ganesh

    IPC分类号： C07D50136

    CPC分类号： C07D501/00

    摘要： The present invention relates to preparation of Ceftiofur acid of formula (I), and its pharmaceutically acceptable salts. The process includes the steps of (i) condensing an activated derivative of wherein the activated derivative is selected from acid halides, mixed anhydrides and active amides, and wherein X represents halogen atom selected from chlorine and bromine, with silylated derivative of wherein R represents p-methoxybenzyl, p-nitrobenzyl or diphenylmethyl in the presence of a solvent at −40° C. to 0° C. to produce (ii) cyclising (V) with thiourea in the presence of water miscible solvent and sodium acetate at room temperature to produce cephalosporin (iii) deesterifying (VI) to produce (I) using anisole/trifluoroacetic acid, phenol/trifluoroacetic acid or formic acid at 0° C. to 10° C. and, if desired, (iv) converting (I), to its pharmaceutically acceptable salt. The invention also relates to intermediates (V) and (VI)

    摘要翻译： 本发明涉及式（I）的头孢噻呋及其药学上可接受的盐的制备。 该方法包括以下步骤：（i）将活化衍生物的活化衍生物缩合为选自酰基卤，混合酸酐和活性酰胺，并且其中X表示选自氯和溴的卤素原子，其中R的甲硅烷基化衍生物代表对甲氧基苄基 ，对硝基苄基或二苯基甲基在溶剂存在下，在-40℃至0℃下，在室温下在水混溶性溶剂和乙酸钠存在下，用硫脲环化（V）以产生头孢菌素 （iii）在0℃至10℃下使用苯甲醚/三氟乙酸，苯酚/三氟乙酸或甲酸进行脱酯（VI）以制备（I），如果需要，（iv）将（I）转化为 药学上可接受的盐。 本发明还涉及中间体（V）和（VI）

    Process for the preparation of Cefditoren
    4.
    发明授权
    Process for the preparation of Cefditoren 失效
    头孢托仑的制备方法

    公开(公告)号：US07459550B2

    公开(公告)日：2008-12-02

    申请号：US10563371

    申请日：2004-07-03

    申请人： Kumar Sahoo Prabhat ,  Anandam Vempali ,  Sivakumaran Sundaravadivelan ,  Nagesh Ganesh Praveen ,  Manikrao Waghdare Vittal ,  Balawant Deshpande Pandurang ,  Kumar Luthra Parven ,  Ramesh Sathe Pratik

    发明人： Kumar Sahoo Prabhat ,  Anandam Vempali ,  Sivakumaran Sundaravadivelan ,  Nagesh Ganesh Praveen ,  Manikrao Waghdare Vittal ,  Balawant Deshpande Pandurang ,  Kumar Luthra Parven ,  Ramesh Sathe Pratik

    IPC分类号： C07D501/24

    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。