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公开(公告)号：EP0627433B1
公开(公告)日：2003-03-05
申请号：EP94901045.8
申请日：1993-12-07
发明人： URAWA, Yoshio 16-27, Konoike Ohkaryo , FURUKAWA, Ken Residence Hiro 202 , SHIMIZU, Toshikazu Konoike Ohkaryo , YAMAGISHI, Yoji , TSURUGI, Tomio 1-1044-130, Toyosatodai , ICHINO, Tomio 2333-197, Kyuchu
IPC分类号： C07D471/04 , C07D213/75 , C07D263/10 , C07D263/14 , C07D413/12 , C07F7/18 , C07C63/06 , C07C309/65 , C07C309/73 , C07C65/105 , C07C69/76
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 invention provides an industrially excellent process for producing a 2-alkyl-3-(biphenyl-4-yl)-methyl-3H-imidazo[4.5-b]pyridine derivative represented by general formula (II), serving as a precursor of the angiotensin II receptor antagonist useful as an antihypertensive, a biphenyl derivative serving as a precursor of the substituent of the imidazopyridine derivative, a process for producing the biphenyl derivative, and an intermediate useful for producing the biphenyl derivative. The imidazopyridine derivative (II) can be produced in a high yield according to the process of the invention by subjecting a 2-amino-5-halogeno-3-nitropyridine derivative to amidation, N-alkylation and reductive cyclization. This process is industrially excellent, because the halogen atom introduced into the 5-position as a protective group in the nitration step can be eliminated simultaneously in the subsequent step. The above biphenyl derivative is excellent in reactivity and product purity, thus being an intermediate suitable for industrial production.
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2.发明公开PROCESS FOR PRODUCING IMIDAZOPYRIDINE DERIVATIVE AND INTERMEDIATE 失效VERFAHREN ZUR HERSTELLUNG VON IMIDAZOPYRIDINDERIVATEN UND ZWISCHENPRODUKTE。
公开(公告)号：EP0627433A1
公开(公告)日：1994-12-07
申请号：EP94901045.8
申请日：1993-12-07
发明人： URAWA, Yoshio 16-27, Konoike Ohkaryo , FURUKAWA, Ken Residence Hiro 202 , SHIMIZU, Toshikazu Konoike Ohkaryo , YAMAGISHI, Yoji , TSURUGI, Tomio 1-1044-130, Toyosatodai , ICHINO, Tomio 2333-197, Kyuchu
IPC分类号： C07D471/04 , C07D213/75 , C07D263/10 , C07D263/14 , C07D413/12 , C07F7/18 , C07C63/06 , C07C309/65 , C07C309/73 , C07C65/105 , C07C69/76
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 invention provides an industrially excellent process for producing a 2-alkyl-3-(biphenyl-4-yl)-methyl-3H-imidazo[4,5-b]pyridine derivative represented by general formula (II), serving as a precursor of the angiotensin II receptor antagonist useful as an antihypertensive, a biphenyl derivative serving as a precursor of the substituent of the imidazopyridine derivative, a process for producing the biphenyl derivative, and an intermediate useful for producing the biphenyl derivative. The imidazopyridine derivative (II) can be produced in a high yield according to the process of the invention by subjecting a 2-amino-5-halogeno-3-nitropyridine derivative to amidation, N-alkylation and reductive cyclization. This process is industrially excellent, because the halogen atom introduced into the 5-position as a protective group in the nitration step can be eliminated simultaneously in the subsequent step. The above biphenyl derivative is excellent in reactivity and product purity, thus being an intermediate suitable for industrial production.
摘要翻译： 本发明提供了制备用作前体的通式（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优异的方法 可用作抗高血压药的血管紧张素II受体拮抗剂，作为咪唑并吡啶衍生物的取代基的前体的联苯衍生物，联苯衍生物的制备方法和可用于制备联苯衍生物的中间体。 根据本发明的方法，可以通过使2-氨基-5-卤代-3-硝基吡啶衍生物进行酰胺化，N-烷基化和还原环化，以高产率制备咪唑并吡啶衍生物（II）。 该工艺在工业上是优异的，因为在后续步骤中可以同时消除在硝化步骤中作为保护基引入5位的卤素原子。 上述联苯衍生物的反应性和产物纯度优异，因此是适于工业生产的中间体。
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