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2. 发明公开

EP0945434A1 PROCESS FOR PRODUCING HALOGENATED HETEROARYL COMPOUNDS 失效
标题翻译： VERFAHREN ZUR HERSTELLUNG VON HALOGENIERTEN HETEROARYLVERBINDUNGEN
公开(公告)号：EP0945434A1
公开(公告)日：1999-09-29
申请号：EP97946159.7
申请日：1997-12-09
申请人： BANYU PHARMACEUTICAL CO., LTD.
发明人： OKADA, Shigemitsu, Banyu Pharm. Co. Ltd Okazaki st , USHIJIMA, Ryosuke, Banyu Pharm. Co. Ltd , ISHIKAWA, Kiyofumi, Banyu Pharm. Co Ltd R&D Lab
IPC分类号： C07D213/61 , C07D215/48 , C07D239/34 , B01J27/16
CPC分类号： C07D213/79 , C07D213/61 , C07D213/85 , C07D215/48 , C07D241/44
摘要： The present invention relates to a process for producing a compound represented by the following general formula [II]:
wherein X is a halogen atom, each of A 1 , A 2 and A 3 may be identical or different, is a carbon atom or a nitrogen atom, provided that at least one of A 1 , A 2 and A 3 is a nitrogen atom, and each of R 1 , R 2 , R 3 and R 4 may be identical or different, is a hydrogen atom, a lower alkyl group, a cyano group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, a hydroxyl group or an amino-(lower alkyl) group, provided that in cases where R 1 and R 2 are adjacent to each other, R 1 and R 2 may be combined with each other to form a 5- or 6-membered ring which may carry on the ring thereof one substituent selected from the group consisting of a lower alkyl group, a nitrile group, a carboxyl group, a lower alkoxycarbonyl group, a carbamoyl group, a halogen atom, a nitro group, a hydroxyl group and an amino-(lower alkyl) group; characterized by reacting a compound represented by the following general formula [I]:
wherein A 1 , A 2 , A 3 , R 1 , R 2 , R 3 and R 4 are as defined above, with a quaternary ammonium halide in the presence of phosphorus pentoxide.
摘要翻译：本发明涉及一种制备由以下通式表示的化合物的方法：其中X是卤素原子，A 1，A 2和A 3中的每一个可以相同或不同是碳原子或氮原子，条件是A 1，A 2和A 3中的至少一个为氮原子，R 1，R 2，R 3， 3>和R 4可以相同或不同，是氢原子，低级烷基，氰基，羧基，低级烷氧基羰基，氨基甲酰基，卤素原子，硝基，羟基基团或氨基 - （低级烷基）基团，条件是在R 1和R 2彼此相邻的情况下，R 1和R 2可以彼此结合形成5 - 或6元环，其可以带有一个选自低级烷基，腈基，羧基，低级烷氧基羰基，氨基甲酰基，卤素原子，硝基的取代基，羟基和氨基 - （低级烷基）基团; 其特征在于使由以下通式表示的化合物：其中A 1，A 2，A 3，R 1，R 2，R 3和R 4， >如上定义，在五氧化二磷的存在下与季铵卤化物反应。

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