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    Process for the preparation of 3-methylcepham derivatives
    1.
    发明授权
    Process for the preparation of 3-methylcepham derivatives 有权
    3-甲基头孢衍生物的制备方法

    公开(公告)号：US07273935B2

    公开(公告)日：2007-09-25

    申请号：US10922992

    申请日：2004-08-23

    申请人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

    发明人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Andrew Gnanaprakasam ,  Kanagaraj Sureshkumar

    IPC分类号： C07D501/08 ,  C07D499/063

    CPC分类号： C07D501/00 ,  C07D499/00

    摘要： A process for the preparation of 3-methylcepham-4-carboxylate of the formula (I). wherein R2 and R3 may be same or different and represent hydrogen, halogen, amino, alkyl, phenacetamido, substituted acetamido, phthalimido with a proviso that both R2 and R3 are not NH2, phenacetamido, phthalimido and the like; R1 represents a lower alkyl, p-methoxybenzyl, p-nitrobenzyl, o-nitrobenzyl, o-methoxybenzyl, o-chlorobenzyl or diphenylmethyl group, or a suitable ester residue which can be deprotected at a latter stage, L represents a leaving group; which comprises cyclizing the compound of formula (III) using a cyclizing agent in the presence of organic or inorganic nitrites and a solvent at a temperature in the range of −40° C. to +60° C. to obtain compound of formula (I).

    摘要翻译： 制备式（I）的3-甲基头孢-4-羧酸酯的方法。 其中R 2和R 3可以相同或不同，表示氢，卤素，氨基，烷基，苯乙酰氨基，取代的乙酰氨基，苯二甲酰亚氨基，条件是R“ 2和R 3不是NH 2，苯乙酰氨基，邻苯二甲酰亚氨基等; R 1表示低级烷基，对甲氧基苄基，对硝基苄基，邻硝基苄基，邻甲氧基苄基，邻氯苄基或二苯基甲基或适合的酯残基，其可以在后一阶段脱保护 L表示离去基团; 其包括在有机或无机亚硝酸盐和溶剂的存在下，在-40℃至+ 60℃的温度下，使用环化剂环化式（III）的化合物，得到式（I ）。

    Process for the preparation of cephalosporin antibiotic
    2.
    发明授权
    Process for the preparation of cephalosporin antibiotic 失效
    制备头孢菌素抗生素的方法

    公开(公告)号：US07339055B2

    公开(公告)日：2008-03-04

    申请号：US10922991

    申请日：2004-08-23

    申请人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Velladurai Hero

    发明人： Pandurang Balwant Deshpande ,  Udayampalayam Palanisamy Senthilkumar ,  Velladurai Hero

    IPC分类号： C07D501/56 ,  C07D501/36 ,  C07D501/34 ,  C07D501/22

    CPC分类号： C07D501/00

    摘要： A process for the preparation of cephalosporin antibiotic of the formula (I) which comprises: (i) activating the compound of formula (III) as acid halide in an organic solvent (ii) treating the reaction mass obtained from step (i) with water (iii) separating the organic layer containing the reactive derivative of formula (III) and condensing it with 7-amino cephalosporin derivative by maintaining the pH in the range 5.0-10.0 using an inorganic base of the formula (XV), and iv) cyclizing the compound of formula (XVI) with thiourea in the presence of solvent and salt of organic or inorganic acid at a temperature in the range of −50 to +50° C. to produce compound of formula (I).

    摘要翻译： 一种制备式（I）的头孢菌素抗生素的方法，其包括：（i）在有机溶剂中活化式（III）化合物作为酰卤;（ii）用水处理步骤（i）获得的反应物质 （iii）使用式（XV）的无机碱将pH维持在5.0-10.0的范围内，分离含有式（III）的活性衍生物的有机层，并将其与7-氨基头孢菌素衍生物缩合，以及iv） 式（ⅩⅥ）化合物与硫脲在有机或无机酸的存在下，在-50至+ 50℃的温度范围内存在下反应生成式（I）化合物。

    Process for the preparation of Tazobactam in pure form
    4.
    发明授权
    Process for the preparation of Tazobactam in pure form 失效
    以纯形式制备他唑巴坦的方法

    公开(公告)号：US07417143B2

    公开(公告)日：2008-08-26

    申请号：US11098526

    申请日：2005-04-05

    申请人： Andrew Gnanaprakasam ,  Udayampalayam Palanisamy Senthilkumar ,  Gaddam Om Reddy

    发明人： Andrew Gnanaprakasam ,  Udayampalayam Palanisamy Senthilkumar ,  Gaddam Om Reddy

    IPC分类号： C07D499/18

    CPC分类号： C07D499/00

    摘要： An improved process for the purification of tazobactam or its derivatives of the formula (I) wherein R represents hydrogen, C1-C6alkyl, p-methoxybenzyl, o-nitrobenzyl, p-nitrobenzyl, o-chlorobenzyl, benzyl or diphenylmethyl, which comprises the steps of: i) slurrying the compound of formula (I) containing the impurity of the formula (V) using a solvent in the presence or absence of tartaric acid with or without the presence of water at 20-50° C. and ii) isolating the compound of formula (I) in pure form.

    摘要翻译： 用于纯化式（I）的他唑巴坦或其衍生物的改进方法，其中R表示氢，C 1 -C 6烷基，对甲氧基苄基，邻 - 硝基苄基 ，对硝基苄基，邻氯苄基，苄基或二苯基甲基，其包括以下步骤：i）在存在或不存在酒石酸的情况下，使用溶剂将含有式（V）的杂质的式（I）化合物在酒石酸存在或不存在下， 或在20-50℃下不存在水，和ii）以纯形式分离式（I）化合物。