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公开(公告)号：EP1285917A1
公开(公告)日：2003-02-26
申请号：EP01926119.7
申请日：2001-05-02
发明人： AKI, Shinji , KURIMURA, Muneaki , NISHI, Takao , MINAMIKAWA, Jun-ichi , TOMINAGA, Michiaki , FUKUYAMA, Norihiro , YAMAMOTO, Akihiro
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , A61K31/4709
摘要： The present invention provides a process for producing carbostyril derivatives (I) which are known to be useful as medical drug such as antithrombotic agent, cerebral circulation improver, anti-inflammatory agent, antiulcer agent, etc. in a high yield and a high purity. The carbostyril derivatives (I) can be produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase transfer catalyst.
摘要翻译： 本发明提供已知可高收率且高纯度地用作抗血栓剂，脑循环改善剂，消炎剂，抗溃疡剂等医药品的喹诺酮衍生物（I）的制造方法。 喹诺酮衍生物（I）可以通过使喹诺酮衍生物（II）与四唑衍生物（III）在相转移催化剂存在下反应来制备。
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2.发明授权
公开(公告)号：EP2528896B1
公开(公告)日：2014-08-27
申请号：EP11706939.3
申请日：2011-01-28
发明人： YAMAMOTO, Akihiro , SHINHAMA, Koichi , FUJITA, Nobuhisa , AKI, Shinji , OGASAWARA, Shin , UTSUMI, Naoto
IPC分类号： C07D211/46 , C07D405/12 , C07D498/04
CPC分类号： C07D211/46 , C07D405/12 , C07D498/04
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公开(公告)号：EP1727782B1
公开(公告)日：2012-08-22
申请号：EP05727512.5
申请日：2005-03-25
发明人： KIYOKAWA, Hiroshi , AKI, Shinji
IPC分类号： C07C213/02 , C07D295/08 , C07D211/46 , C07C215/82 , C07C215/76
CPC分类号： C07D295/096 , C07C213/02 , C07C215/76 , C07C215/82
摘要： The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.
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4.发明公开
公开(公告)号：EP2528896A1
公开(公告)日：2012-12-05
申请号：EP11706939.3
申请日：2011-01-28
发明人： YAMAMOTO, Akihiro , SHINHAMA, Koichi , FUJITA, Nobuhisa , AKI, Shinji , OGASAWARA, Shin , UTSUMI, Naoto
IPC分类号： C07D211/46 , C07D405/12 , C07D498/04
CPC分类号： C07D211/46 , C07D405/12 , C07D498/04
摘要： An object of the present invention is to provide a method for producing an oxazole compound in a high yield. The object can be achieved by a compound represented by Formula (11): wherein R
1 is a hydrogen atom or lower-alkyl group; R
2 is a 1-piperidyl group substituted at the 4-position with a substituent selected from (A1a) a phenoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1b) a phenoxy-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkyl groups, (A1c) a phenyl-substituted lower-alkoxy lower-alkyl group substituted on the phenyl moiety with halogen, (A1d) a phenyl-substituted lower-alkyl group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups, (A1e) an amino group substituted with a phenyl group substituted with one or more halogen-substituted lower-alkoxy groups, and a lower-alkyl group, and (A1f) a phenyl-substituted lower-alkoxy group substituted on the phenyl moiety with one or more halogen-substituted lower-alkoxy groups; n is an integer from 1 to 6; and X
3 is an organic sulfonyloxy group.-
公开(公告)号：EP1727782A1
公开(公告)日：2006-12-06
申请号：EP05727512.5
申请日：2005-03-25
发明人： KIYOKAWA, Hiroshi , AKI, Shinji
IPC分类号： C07C213/02 , C07D295/08 , C07D211/46 , C07C215/82 , C07C215/76
CPC分类号： C07D295/096 , C07C213/02 , C07C215/76 , C07C215/82
摘要： The present invention provides an industrially advantageous method of producing aminophenol compounds represented by the formula (1) by a simple and easy procedure at a high yield and a high purity. The present invention provides a method of producing an aminophenol compound represented by the formula (1): (wherein each of R1 and R2, which may be the same or different, is a hydrogen atom, a substituted or unsubstituted lower alkyl group or the like; R1 and R2, taken together with the adjacent nitrogen atom, may form a 5- or 6-membered heterocycle with or without other intervening heteroatoms; the heterocycle may be substituted by 1 to 3 substituents selected from the group consisting of a hydroxyl group, a substituted or unsubstituted lower alkyl group, a substituted or unsubstituted aryl group, a substituted or unsubstituted aryloxy group and the like; and the hydroxyl group in the formula (1) is substituted on the 2- or 4-position to the amino group on the phenyl ring), which comprises allowing a cyclohexanedione compound represented by the formula (2) to react with an amine compound represented by the formula (3) (wherein R1 and R2 are as defined above), under a neutral or basic condition.
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公开(公告)号：EP1285917B1
公开(公告)日：2004-12-29
申请号：EP01926119.7
申请日：2001-05-02
发明人： AKI, Shinji , KURIMURA, Muneaki , NISHI, Takao , MINAMIKAWA, Jun-ichi , TOMINAGA, Michiaki , FUKUYAMA, Norihiro , YAMAMOTO, Akihiro
IPC分类号： C07D401/12
CPC分类号： C07D401/12 , A61K31/4709
摘要： A novel process for producing in high yield a high-purity carbostyril derivative (I), which is known to be useful as a medicine such as an antithrombotic agent, cerebral vasodilator, antiinflammatory agent, or antiulcer agent. The carbostyril derivative (I) is produced by reacting a carbostyril derivative (II) with a tetrazole derivative (III) in the presence of a phase-transfer catalyst. (I) (II) (III)
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