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    PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL
    4.
    发明申请
    PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL 审中-公开
    制备CANDESARTAN CILEXETIL的方法

    公开(公告)号：US20100210853A1

    公开(公告)日：2010-08-19

    申请号：US12678316

    申请日：2008-06-24

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Matta Ramakrishna Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Matta Ramakrishna Reddy

    IPC分类号： C07D257/04

    CPC分类号： C07D403/10

    摘要： There was provided a process for preparing candesartan cilexetil, the said process comprises hydrogenating a solution of trityl candesartan cilexetil in an alcohol with hydrogen in the presence of a palladium catalyst. Mixture of toluene and methanol was added to 1-(Cyclohexyloxy carbonyloxy)ethyl-2-ethoxy-1-[[2′-(N-triphenylmethyltetrazole-5-yl)biphenyl-4-yl]methyl]benzimidazole-7-carboxylate and hydrogenated at room temperature with hydrogen at atmospheric pressure in the presence of palladium on carbon until the hydrogen uptake was ceased. Filtered over celite bed, washed the bed with a mixture of toluene and methanol, filtrate was collected and concentrated. Co-distilled with acetonitrile, acetonitrile was added, stirred at room temperature, cooled to 0° C. stirred, filtered, washed with chilled acetonitrile and dried to get candesartan cilexetil.

    摘要翻译： 提供了一种制备坎地沙坦酯的方法，所述方法包括在钯催化剂存在下，用氢气将三苯甲基坎地沙坦酯在醇中氢化。 将甲苯和甲醇的混合物加入到1-（环己氧基羰基氧基）乙基-2-乙氧基-1 - [[2' - （N-三苯基甲基四唑-5-基）联苯-4-基]甲基]苯并咪唑-7-羧酸甲酯和 在大气压下，在钯碳存在下，在室温下氢化直到氢吸收停止。 在硅藻土床上过滤，用甲苯和甲醇的混合物洗涤床，收集滤液并浓缩。 用乙腈共蒸馏，加入乙腈，在室温下搅拌，冷却至0℃，搅拌，过滤，用冷乙腈洗涤，干燥得到坎地沙坦酯。

    PROCESS FOR FEBUXOSTAT
    5.
    发明申请
    PROCESS FOR FEBUXOSTAT 审中-公开
    FEBUXOSTAT的过程

    公开(公告)号：US20140112992A1

    公开(公告)日：2014-04-24

    申请号：US14123875

    申请日：2012-05-21

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Matta Ramakrishna Reddy ,  Bandi Vamsi Krishna

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Dasari Muralidhara Reddy ,  Matta Ramakrishna Reddy ,  Bandi Vamsi Krishna

    IPC分类号： C07D277/56 ,  A61K31/426

    CPC分类号： C07D277/56 ,  A61K31/426

    摘要： The present invention provides a process for the preparation of 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention also provides a process for the preparation of 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention further provides novel crystalline Forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides febuxostat crystalline particles having a mean particle size of less than about 25 μm, the methods for the manufacture of said crystalline particles, and pharmaceutical compositions comprising said crystalline particles.

    摘要翻译： 本发明提供了制备2-（4-羟基苯基）-4-甲基噻唑-5-羧酸乙酯的方法。 本发明还提供了制备2-（3-甲酰基-4-羟基苯基）-4-甲基噻唑-5-甲酸乙酯的方法。 本发明进一步提供了新型的布氏抑菌素的结晶形式，其制备方法和包含它们的药物组合物。 本发明还提供平均粒度小于约25μm的Febustostat结晶颗粒，制备所述结晶颗粒的方法和包含所述结晶颗粒的药物组合物。

    PROCESS FOR PURE IRBESARTAN
    6.
    发明申请
    PROCESS FOR PURE IRBESARTAN 审中-公开
    纯IRBESARTAN的工艺

    公开(公告)号：US20100234614A1

    公开(公告)日：2010-09-16

    申请号：US12306721

    申请日：2007-12-07

    申请人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Matta Ramakrishna Reddy

    发明人： Bandi Parthasaradhi Reddy ,  Kura Rathnakar Reddy ,  Rapolu Raji Reddy ,  Dasari Muralidhara Reddy ,  Matta Ramakrishna Reddy

    IPC分类号： C07D257/04 ,  C07D487/10

    CPC分类号： C07D403/10 ,  C07D235/02

    摘要： The present invention provides an improved and commercially viable process for preparation of irbesartan intermediate, 1-[(2′-cyanobiphenyl-4-yl)methyl]-2-n-butyl-4-spirocyclopentane-2-imidazolin-5-one, substantially free of 1-[(2′-cyanobiphenyl-4-yl)methyl]-2-n-propyl-4-spirocyclopentane-2-imidazolin-5-one impurity, thereby producing irbesartan substantially free of the undesired propyl analog impurity, namely 2-propyl-3-[[2′-(1H-tetrazol-5-yl)[1,1′-biphenyl]-4-yl]methyl]-1,3 -diazaspiro[4.4]non-1-en-4-one. The present invention also provides a process for preparation of irbesartan substantially free of tin content. The present invention further provides a commercially viable process for preparation of irbesartan in high purity and in high yield.

    摘要翻译： 本发明提供了制备厄贝沙坦中间体1 - [（2'-氰基联苯-4-基）甲基] -2-正丁基-4-螺环戊烷-2-咪唑啉-5-酮的改进和商业上可行的方法， 基本上不含1 - [（2'-氰基联苯-4-基）甲基] -2-正丙基-4-螺环戊烷-2-咪唑啉-5-酮杂质，从而制备基本上不含不希望的丙基类似杂质的厄​​贝沙坦， 即2-丙基-3 - [[2' - （1H-四唑-5-基）[1,1'-联苯] -4-基]甲基] -1,3-二氮杂螺[4.4]壬-1-烯 -4-one。 本发明还提供了制备基本上不含锡含量的厄贝沙坦的方法。 本发明进一步提供了以高纯度和高产率制备厄贝沙坦的商业上可行的方法。