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    Process for preparation of Irbesartan
    3.
    发明授权
    Process for preparation of Irbesartan 失效
    厄贝沙坦制备方法

    公开(公告)号：US07652147B2

    公开(公告)日：2010-01-26

    申请号：US11406919

    申请日：2006-04-19

    申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Dhiraj Mohansinh Rathod ,  Hitesh Kantilal Patel ,  Pinky Tarak Parikh

    发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra ,  Dhiraj Mohansinh Rathod ,  Hitesh Kantilal Patel ,  Pinky Tarak Parikh

    IPC分类号： C07D257/00 ,  C07D403/00

    CPC分类号： C07C231/02 ,  C07C2601/08 ,  C07D403/10 ,  C07C233/52

    摘要： A process for the preparation of Irbesartan of formula (I) using the steps of: (i) reacting 4′ aminomethyl-2-cyano biphenyl of formula (VI) with 1-veleramido cyclopentane carboxylic acid of formula (V) in an organic solvent and in the presence of an acid, without activating the —COOH group of compound of formula (V) to give 1-(2′cyanobiphenyl-4-yl-methylaminocarbonyl)-1-pentanoylamino cyclopentane of formula (VII). converting the compound of formula (VII) obtained in step (i) to Irbesartan of formula (I) by reacting the compound of the formula (VII) with tributyl tin azide in o-xylene to give Irbesartan of formula (I).

    摘要翻译： 使用以下步骤制备式（I）的厄贝沙坦的方法：（i）使式（VI）的4'-氨基甲基-2-氰基联苯与式（V）的1-维拉酰氨基环戊烷羧酸在有机溶剂 并且在酸存在下，不活化式（Ⅴ）化合物的-COOH基，得到式（Ⅶ）的1-（2'-氰基联苯-4-基 - 甲基氨基羰基）-1-戊酰基氨基环戊烷。 通过使式（Ⅶ）化合物与叠氮化三丁基锡在邻二甲苯中反应，得到式（ⅰ）中得到的式（Ⅶ）化合物转化成式（I）所示的厄贝沙坦，得到式（I）的厄贝沙坦。

    Thioester derivatives of thiazolyl acetic acid and their use in the preparation of cephalosporin compounds
    7.
    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。

    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：US06388070B1

    公开(公告)日：2002-05-14

    申请号：US09754302

    申请日：2001-01-05

    申请人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

    发明人： Pandurang Balwant Deshpande ,  Parven Kumar Luthra

    IPC分类号： C07D41712

    CPC分类号： C07D417/12 ,  C07D501/00 ,  Y02P20/55

    摘要： The present invention provides novel thioester derivatives of thiazolyl acetic acid of the general formula (I), wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; and R2 represents C1-C4 alkyl or phenyl. The invention also provides a method for preparation of the thioester derivatives and reaction of the thioester derivatives with cephem carboxylic acids to produce cephalosporin antibiotic compounds having general formula (II), wherein, R1 represents H, trityl, CH3, or CRaRbCOOR3, in which Ra and Rb, independently of one another, represents hydrogen or methyl and R3 represents H or C1-C7 alkyl; R4 is CH3, —CH═CH2, CH2OCH3, CH2OCOCH3, and R5 is H or a salt or a carboxylic protecting group, comprising, acylating a compound of formula (III), wherein, R4 and R5 are defined as above, and R6 is H or trimethylsilyl; with a compound of formula (I).

    摘要翻译： 本发明提供通式（I）的噻唑基乙酸的新型硫酯衍生物，其中R1表示H，三苯甲基，CH3或CRaRbCOOR3，其中Ra和Rb彼此独立地表示氢或甲基，R3表示 H或C 1 -C 7烷基; 并且R 2表示C 1 -C 4烷基或苯基。 本发明还提供了硫酯衍生物的制备方法和硫酯衍生物与头孢烯羧酸反应产生具有通式（II）的头孢菌素抗生素化合物，其中R1表示H，三苯甲基，CH3或CRaRbCOOR3，其中Ra 和R b彼此独立地表示氢或甲基，R 3表示H或C 1 -C 7烷基; R4是CH3，-CH = CH2，CH2OCH3，CH2OCOCH3，R5是H或盐或羧基保护基，其包括酰化式（III）化合物，其中R4和R5定义如上，R6是 H或三甲基甲硅烷基;与式（I）的化合物反应。

    Process for the preparation of cefoxitin
    10.
    发明授权
    Process for the preparation of cefoxitin 失效
    头孢西丁的制备方法

    公开(公告)号：US07662955B2

    公开(公告)日：2010-02-16

    申请号：US10548888

    申请日：2003-12-31

    申请人： Pandurang Balwant Deshpande ,  Bhausaheb Pandharinath Khadangale

    发明人： Pandurang Balwant Deshpande ,  Bhausaheb Pandharinath Khadangale

    IPC分类号： C07D501/57

    CPC分类号： C07D501/34

    摘要： A process for the preparation of cefoxitin of formula (I) The process includes treating the compound of formula (II) with a halogenating agent in an organic solvent, followed by treatment with alkali/alkaline earth metal methoxide at a temperature in the range of −100° C. to 0° C. The product formed is then isolated as an organic amine salt of the formula (III), The salt of formula (III) is treated with a base in the presence of solvent at a temperature in the range of −75 to 10° C., the product formed is isolated as an organic amine salt of the formula (IV) The compound of formula (IV) is carbamoylated with isocyanate of formula (V) RNCO  (V) in the presence of a solvent at a temperature in the range of −60° C. to 10° C., and isolating to get cefoxitin of the formula (I).

    摘要翻译： 制备式（I）头孢西丁的方法该方法包括用有机溶剂中的卤化剂处理式（II）化合物，然后在碱金属/碱土金属甲醇盐的温度范围内处理， 然后将所形成的产物作为式（III）的有机胺盐分离。式（III）的盐在溶剂存在下在碱的存在下在一定温度范围内用碱处理 分离出形成的产物作为式（IV）的有机胺盐。式（Ⅳ）化合物在式（Ⅳ）化合物的存在下在式 溶剂，温度范围为-60℃至10℃，并分离得到式（I）的头孢西丁。