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    Intermediates for substituted biphenylmethylmidazopyridine angiotensin II antagonists
    3.
    发明授权
    Intermediates for substituted biphenylmethylmidazopyridine angiotensin II antagonists 失效
    取代联苯甲基咪唑并吡啶血管紧张素II拮抗剂的中间体

    公开(公告)号：US5559236A

    公开(公告)日：1996-09-24

    申请号：US471465

    申请日：1995-06-06

    申请人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    发明人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    IPC分类号： C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/73 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04 ,  C07D413/10

    CPC分类号： C07D213/73 ,  C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo-[4,5-b]pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous. Further, the biphenyl derivative of the present invention is excellent in reactivity and purity of the product, thus being an intermediate suitable for the industrial production.

    摘要翻译： 本发明提供了制备由下式（II）表示的2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物的工业上有利的方法，其为前体 可用作抗高血压药物的血管紧张素II受体的拮抗剂，作为吡啶衍生物的取代基的前体的联苯衍生物，其制备方法和用于制备联苯衍生物的中间体：（II）2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物可以按照本发明从2-氨基 -5-卤代-3-硝基吡啶衍生物通过酰胺化，N-烷基化和还原环化。 在其后进行的步骤中可以同时消除在5位引入作为硝化保护基的卤素原子。 因此，该方法在工业上是有利的。 此外，本发明的联苯衍生物的产物的反应性和纯度优异，因此是适于工业化生产的中间体。

    Intermediates for imidazopyridine derivatives
    4.
    发明授权
    Intermediates for imidazopyridine derivatives 失效
    咪唑并吡啶衍生物的中间体

    公开(公告)号：US5700938A

    公开(公告)日：1997-12-23

    申请号：US468090

    申请日：1995-06-06

    申请人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    发明人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    IPC分类号： C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/73 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04

    CPC分类号： C07D213/73 ,  C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo�4,5-b!pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo�4,5-b!pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous. Further, the biphenyl derivative of the present invention is excellent in reactivity and purity of the product, thus being an intermediate suitable for the industrial production.

    摘要翻译： 本发明提供了制备由下式（II）表示的2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物的工业上有利的方法，其为前体 可用作抗高血压药物的血管紧张素II受体的拮抗剂，作为吡啶衍生物的取代基的前体的联苯衍生物，其制备方法和用于制备联苯衍生物的中间体：（II）2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物可以按照本发明从2-氨基 - 5-卤代-3-硝基吡啶衍生物通过酰胺化，N-烷基化和还原环化。 在其后进行的步骤中可以同时消除在5位引入作为硝化保护基的卤素原子。 因此，该方法在工业上是有利的。 此外，本发明的联苯衍生物的产物的反应性和纯度优异，因此是适于工业化生产的中间体。

    Process for the preparation of imidazopyridine derivatives and intermediates
    6.
    发明授权
    Process for the preparation of imidazopyridine derivatives and intermediates 失效
    咪唑并吡啶衍生物和中间体的制备方法

    公开(公告)号：US5608068A

    公开(公告)日：1997-03-04

    申请号：US471677

    申请日：1995-06-06

    申请人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    发明人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    IPC分类号： C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/73 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04

    CPC分类号： C07D213/73 ,  C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo-[4,5-b]pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous. Further, the biphenyl derivative of the present invention is excellent in reactivity and purity of the product, thus being an intermediate suitable for the industrial production.

    摘要翻译： 本发明提供了制备由下式（II）表示的2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物的工业上有利的方法，其为前体 可用作抗高血压药物的血管紧张素II受体的拮抗剂，作为吡啶衍生物的取代基的前体的联苯衍生物，其制备方法和用于制备联苯衍生物的中间体：（II）2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物可以按照本发明从2-氨基 -5-卤代-3-硝基吡啶衍生物通过酰胺化，N-烷基化和还原环化。 在其后进行的步骤中可以同时消除在5位引入作为硝化保护基的卤素原子。 因此，该方法在工业上是有利的。 此外，本发明的联苯衍生物的产物的反应性和纯度优异，因此是适于工业化生产的中间体。

    Process for the preparation of imidazopyridine derivatives, and intermediates therefore
    8.
    发明授权
    Process for the preparation of imidazopyridine derivatives, and intermediates therefore 失效
    因此制备咪唑并吡啶衍生物的方法和中间体

    公开(公告)号：US5554757A

    公开(公告)日：1996-09-10

    申请号：US468078

    申请日：1995-06-06

    申请人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    发明人： Yoshio Urawa ,  Ken Furukawa ,  Toshikazu Shimizu ,  Yoji Yamagishi ,  Tomio Tsurugi ,  Tomio Ichino

    IPC分类号： C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/73 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04

    CPC分类号： C07D213/73 ,  C07C63/72 ,  C07C65/105 ,  C07C69/732 ,  C07C69/76 ,  C07D213/75 ,  C07D263/10 ,  C07D263/12 ,  C07D263/14 ,  C07D309/12 ,  C07D413/12 ,  C07D471/04 ,  Y02P20/55

    摘要： The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo-[4,5-b]pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous.Further, the biphenyl derivative of the present invention is excellent in reactivity and purity of the product, thus being an intermediate suitable for the industrial production.

    摘要翻译： 本发明提供了制备由下式（II）表示的2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物的工业上有利的方法，其为前体 可用作抗高血压药物的血管紧张素II受体的拮抗剂，作为吡啶衍生物的取代基的前体的联苯衍生物，其制备方法和用于制备联苯衍生物的中间体：（II）2-烷基-3-（联苯-4-基）甲基-3H-咪唑并[4,5-b]吡啶衍生物可以按照本发明从2-氨基 -5-卤代-3-硝基吡啶衍生物通过酰胺化，N-烷基化和还原环化。 在其后进行的步骤中可以同时消除在5位引入作为硝化保护基的卤素原子。 因此，该方法在工业上是有利的。 此外，本发明的联苯衍生物的产物的反应性和纯度优异，因此是适于工业化生产的中间体。