Process for producing 4-dimethyl amino pyridine (4-DMAP)
    5.
    发明授权
    Process for producing 4-dimethyl amino pyridine (4-DMAP) 失效
    制备4-二甲基氨基吡啶(4-DMAP)的方法

    公开(公告)号:US06939972B2

    公开(公告)日:2005-09-06

    申请号:US10407773

    申请日:2003-04-04

    IPC分类号: C07D213/74 C07D213/02

    CPC分类号: C07D213/74

    摘要: An improved process for producing 4-dimethyl amino pyridine is provided. The process comprises quaternizing pyridine with a suitable quaternizing agent in the presence of organic solvent, isolating the resulting salt and aminating the salt, N-[4-pyridyl] pyridinium chloride hydrochloride, with N,N-dimethyl formamide. The resultant reaction mass is hydrolysed in the presence of a base, extracted with an aromatic solvent and distilled under vacuum to produce 4-dimethyl amino pyridine.

    摘要翻译: 提供了一种改进的制备4-二甲基氨基吡啶的方法。 该方法包括在有机溶剂存在下用合适的季铵化剂季铵化吡啶,分离得到的盐,并用N,N-二甲基甲酰胺胺化盐,N- [4-吡啶基]吡啶鎓氯化物盐酸盐。 所得反应物质在碱的存在下水解,用芳族溶剂萃取并在真空下蒸馏以产生4-二甲基氨基吡啶。

    Process for producing 2-(phenyl methyl thio)-3-pyridine carboxylic acid
    7.
    发明授权
    Process for producing 2-(phenyl methyl thio)-3-pyridine carboxylic acid 有权
    2-(苯甲基硫代)-3-吡啶羧酸的制备方法

    公开(公告)号:US07745631B2

    公开(公告)日:2010-06-29

    申请号:US11547407

    申请日:2004-06-17

    IPC分类号: C07D213/02

    CPC分类号: C07D213/80 C07D213/85

    摘要: The invention discloses an improved process for producing an intermediate to produce large quantity of 2-(Phenyl methyl thio)-3-pyridine carboxylic acid. The process comprises reacting 2-chloro-3-cyanopyridine with benzyl mercaptan in presence of a base and an aprotic solvent. The resulting intermediate 2-(phenyl methyl thio)-3-cyanopyridine is hydrolyzed in presence of a base in an autoclave and isolated under acidic condition to get the desired product.

    摘要翻译: 本发明公开了一种生产大量2-(苯基甲基硫代)-3-吡啶羧酸的中间体的改进方法。 该方法包括在碱和非质子溶剂的存在下使2-氯-3-氰基吡啶与苯甲硫醇反应。 得到的中间体2-(苯基甲基硫代)-3-氰基吡啶在高压釜中碱存在下水解,在酸性条件下分离得到所需产物。

    Process For Producing 2-(Phenyl Methyl Thio)-3-Pyridine Carboxylic Acid
    8.
    发明申请
    Process For Producing 2-(Phenyl Methyl Thio)-3-Pyridine Carboxylic Acid 有权
    2-(苯基甲硫基)-3-吡啶羧酸的制备方法

    公开(公告)号:US20080139817A1

    公开(公告)日:2008-06-12

    申请号:US11547407

    申请日:2004-06-17

    IPC分类号: C07D211/04

    CPC分类号: C07D213/80 C07D213/85

    摘要: The invention discloses an improved process for producing an intermediate to produce large quantity of 2-(Phenyl methyl thio)-3-pyridine carboxylic acid. The process comprises reacting 2-chloro-3-cyanopyridine with benzyl mercaptan in presence of a base and an aprotic solvent. The resulting intermediate 2-(phenyl methyl thio)-3-cyanopyridine is hydrolyzed in presence of a base in an autoclave and isolated under acidic condition to get the desired product.

    摘要翻译: 本发明公开了一种生产大量2-(苯基甲基硫代)-3-吡啶羧酸的中间体的改进方法。 该方法包括在碱和非质子溶剂的存在下使2-氯-3-氰基吡啶与苯甲硫醇反应。 得到的中间体2-(苯基甲基硫代)-3-氰基吡啶在高压釜中碱存在下水解,在酸性条件下分离得到所需产物。

    Process for the preparation of azilsartan medoxomil
    9.
    发明授权
    Process for the preparation of azilsartan medoxomil 有权
    制备吖唑烷酯的方法

    公开(公告)号:US09233955B2

    公开(公告)日:2016-01-12

    申请号:US13983521

    申请日:2012-01-24

    IPC分类号: C07D413/10 C07D413/14

    CPC分类号: C07D413/10 C07D413/14

    摘要: The present invention relates to an improved process for the preparation of azilsartan or its esters or salts thereof. Specifically, the invention provides a method for the preparation of highly pure methyl 1-[[2′-(4,5-dihydro-5-oxo-4H-1,2,4-oxa-diazol-3-yl)biphenyl-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylate an intermediate compound of formula (4) for azilsartan medoxomil with reduced content of desethyl impurity. The invention also involves the use of highly pure methyl 1-[[2′-(4,5-dihydro-5-oxo-4H-1,2,4-oxadiazol-3-yl)biphenyl-4-yl]methyl]-2-ethoxy-1H-benzimidazole-7-carboxylate in the preparation of azilsartan or its esters or salts thereof, preferably medoxomil with reduced content of desethyl impurity.

    摘要翻译: 本发明涉及制备吖唑烷或其酯或其盐的改进方法。 具体地说,本发明提供了制备高纯度1 - [[2' - (4,5-二氢-5-氧代-4H-1,2,4-氧杂 - 二唑-3-基)联苯基] 吡啶-4-基]甲基] -2-乙氧基-1H-苯并咪唑-7-羧酸甲酯,其中式(4)的中间体化合物用于脱乙基杂质含量较低的吖唑烷酮。 本发明还涉及使用高纯度的1 - [[2' - (4,5-二氢-5-氧代-4H-1,2,4-恶二唑-3-基)联苯-4-基]甲基] -2-乙氧基-1H-苯并咪唑-7-羧酸乙酯制备吖唑烷或其酯或其盐,优选含有脱乙基杂质含量的内酯。