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    PROCESS FOR PREPARATION OF CANDESARTAN CILEXETIL
    3.
    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。