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    Process for the preparation of a cephalosporin antibiotic
    6.
    发明授权
    Process for the preparation of a cephalosporin antibiotic 失效
    制备头孢菌素抗生素的方法

    公开(公告)号：US07098329B2

    公开(公告)日：2006-08-29

    申请号：US10867723

    申请日：2004-06-16

    申请人： Pandurang Balwant Deshpande ,  Prabhat Kumar Sahoo ,  Anandam Vempali ,  Srinivasu Ghanta

    发明人： Pandurang Balwant Deshpande ,  Prabhat Kumar Sahoo ,  Anandam Vempali ,  Srinivasu Ghanta

    IPC分类号： C07D501/36

    CPC分类号： C07D501/00

    摘要： An improved process for the preparation of ceftriaxone sodium comprising the steps of: i) reacting the 3-cephem derivative of formula (II)  with halo acid derivative of formula (III)  wherein X represents halogen and Y represent halogen in the presence of silylating agent and methylene chloride at −25 to 10° C., to produce (IV), ii) quenching the reaction by pouring the reaction mixture into water or in a aqueous solution of sodium carbonate, iii) preparing sodium salt solution of (IV) by adding sodium carbonate and separating the organic layer, iv) cyclizing the sodium salt of (IV) in the aqueous solution with thiourea at a temperature in the range of 0 to 30° C., v) adjusting the pH to 1.5 to 2.5 to precipitate the ceftriaxone free acid, vi) converting the ceftriaxone free acid to sodium salt using sodium-2-ethyl hexanoate in water and vii) precipitating and isolating the ceftriaxone sodium.

    摘要翻译： 一种用于制备头孢曲松钠的改进方法，包括以下步骤：i）使式（II）的3-头孢烯衍生物与式（III）的卤酸衍生物反应，其中X代表卤素，Y代表甲硅烷基化剂存在下的卤素 和二氯甲烷在-25至10℃下反应，以产生（Ⅳ），ⅱ）通过将反应混合物倒入水中或在碳酸钠水溶液中淬灭反应，ⅲ）制备（Ⅳ）的钠盐溶液 加入碳酸钠并分离有机层，iv）在0至30℃的温度范围内，用硫脲环化水溶液中的（Ⅳ）的钠盐，v）将pH调节至1.5至2.5以沉淀 头孢曲松游离酸，vi）使用2-乙基己酸钠在水中将头孢曲松游离酸转化为钠盐，和vii）沉淀并分离头孢曲松钠。

    Process for the preparation of 3-propenyl cephalosporin DMF solvate
    7.
    发明授权
    Process for the preparation of 3-propenyl cephalosporin DMF solvate 失效
    3-丙烯基头孢菌素DMF溶剂化物的制备方法

    公开(公告)号：US06903211B2

    公开(公告)日：2005-06-07

    申请号：US10315010

    申请日：2002-12-10

    申请人： Pandurang Balwant Deshpande ,  Bhausaheb Pandharinath Khadangale ,  Kumar Gurusamy ,  Ramesh Athmaram Konda

    发明人： Pandurang Balwant Deshpande ,  Bhausaheb Pandharinath Khadangale ,  Kumar Gurusamy ,  Ramesh Athmaram Konda

    IPC分类号： C07D501/00 ,  C07D501/04 ,  C07D501/12 ,  C07D510/22

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： The present invention relates to an improved process for the preparation of cefprozil DMF solvate of formula (I), which is useful for the preparation of cefprozil, comprising: i) reacting a compound of formula (VIII) with acetaldehyde to produce a compound of formula (IX), ii) deesterifying the carboxy protecting group of the compound of formula (IX) using an acid to yield a compound of formula (X), iii) converting the compound of formula (X) to a compound of formula (XI), iv) neutralizing the compound of formula (XI) followed by enzymatic hydrolysis to produce an APCA of formula (V), v) silylating the APCA using a mixture of trimethylsilylchloride and hexamethyldisilazane to produce silylated APCA of formula (XII), and vi) condensing the silylated APCA with a mixed anhydride to produce the DMF solvate compound of formula (I).

    摘要翻译： 本发明涉及用于制备式（I）的头孢丙呋胺溶剂化物的改进方法，其可用于制备头孢丙烯，其包括：i）使式（Ⅷ）化合物与乙醛反应以制备式 （Ⅸ）化合物，ⅱ）使用酸去除式（Ⅸ）化合物的羧基保护基，得到式（Ⅹ）化合物，ⅲ）将式（Ⅹ）化合物转化为式（Ⅺ）化合物， iv）中和式（XI）化合物，然后进行酶水解以产生式（V）的APCA，v）使用三甲基甲硅烷基氯和六甲基二硅氮烷的混合物使APCA甲硅烷基化以制备式（XII）的甲硅烷基化APCA，和vi） 用混合酸酐缩合甲硅烷基化APCA以制备式（I）的DMF溶剂合物。

    Preparation of new intermediates and their use in manufacturing of cephalosporin compounds
    8.
    发明授权
    Preparation of new intermediates and their use in manufacturing of cephalosporin compounds 失效
    新中间体的制备及其在制造头孢菌素化合物中的应用

    公开(公告)号：US06384215B1

    公开(公告)日：2002-05-07

    申请号：US09875043

    申请日：2001-06-07

    申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

    发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

    IPC分类号： C07D27108

    CPC分类号： C07D271/113 ,  C07D501/00

    摘要： The present invention provides new thioester derivatives of 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (I), also, the invention provides a method by which the said thioester derivatives can be prepared by reacting 4-halogeno-2-methoxyimino-3-oxo-butyric acid of the general formula (II) with 2-mercapto-5-substituted-1,3,4-oxadiazoles of the general formula (III) in a solvent, in the presence of DMF/POCl3 and in presence of an organic base and if desired the so obtained thioester derivatives so obtained are reacted with 7-amino-cephem carboxylic acids of the general formula (V) to produce condensed products which are insitu reacted with thiourea to get cephalosporin antibiotic compounds having the general formula (VI).

    摘要翻译： 本发明提供了通式（I）的4-卤代-2-甲氧基亚氨基-3-氧代 - 丁酸的新的硫代酯衍生物，本发明还提供了一种可通过使4- 通式（II）的2-氧代-2-甲氧基亚氨基-3-氧代 - 丁酸与通式（III）的2-巯基-5-取代-1,3,4-恶二唑在溶剂中，在 DMF / POCl 3并在有机碱的存在下，如果需要，如此得到的硫酯类衍生物与通式（Ⅴ）的7-氨基头孢烯羧酸反应，生成与硫脲本身反应得到头孢菌素的缩合产物 具有通式（VI）的抗生素化合物。