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    &bgr;-lactam production
    2.
    发明授权
    &bgr;-lactam production 失效
    β-内酰胺生产

    公开(公告)号：US06777549B2

    公开(公告)日：2004-08-17

    申请号：US10119548

    申请日：2002-04-10

    申请人： Benjamin Gerlach ,  Johannes Ludescher ,  Klaus Totschnig

    发明人： Benjamin Gerlach ,  Johannes Ludescher ,  Klaus Totschnig

    IPC分类号： C07D50136

    CPC分类号： C07D501/00 ,  C07F7/10 ,  C07F7/1804 ,  C07F7/1896

    摘要： A process for the production of a compound of formula comprising i) silylating a compound of formula then reacting a resulting with a compound of formula R′BS—X′  IVB wherein R′B is hydrogen or trialkysilyl and X′ is as defined above, in the presence of a compound of formula wherein R2, R3 and R4 independently of each another are aryl or alkyl, and R5 is alkyl, perfluorinated alkyl, or aryl; and isolating the desired product.

    摘要翻译： 制备化学式的化合物的方法）甲磺酰化所得化合物与式Ⅳ所得化合物的反应是氢或三烷基甲硅烷基，X'如上所定义，在甲醛化合物的存在下，R2，R3 和R 4彼此独立地是芳基或烷基，R 5是烷基，全氟化烷基或芳基; 拆分所需产品。

    Method for the preparation of ceftiofur sodium and its intermediates
    4.
    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）

    Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
    8.
    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。

    Process for the preparation of furaca
    10.
    发明授权
    Process for the preparation of furaca 失效
    羊草制备工艺

    公开(公告)号：US06476220B2

    公开(公告)日：2002-11-05

    申请号：US09902512

    申请日：2001-07-09

    申请人： Uthira Kumar ,  Meenakshisunderam Sivakumaran ,  Vijay Kumar Handa

    发明人： Uthira Kumar ,  Meenakshisunderam Sivakumaran ,  Vijay Kumar Handa

    IPC分类号： C07D50136

    CPC分类号： C07D501/00

    摘要： A process is disclosed for the preparation of 7-amino-3-(2-furanylcarbonylthiomethyl)-3-cephem-4-carboxylic acid (also known as Furaca). The process comprises of the steps of reacting 7-aminocephalosporanic acid with a mixture of 2-thiofuric acid and Boron Trifluoride in a solvent and precipitating Furaca as a solid.

    摘要翻译： 公开了制备7-氨基-3-（2-呋喃基羰基硫甲基）-3-头孢烯-4-羧酸（也称为Furaca）的方法。 该方法包括以下步骤：使7-氨基头孢烷酸与2-硫代磷酸和三氟化硼的混合物在溶剂中反应并使Furaca固体沉淀。