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公开(公告)号:EP0406438A1
公开(公告)日:1991-01-09
申请号:EP90900359.2
申请日:1989-12-25
申请人: Kowa Company. Ltd.
发明人: KAWAMURA, Kiyoshi , OTA, Tomio
IPC分类号: C07D301/28
CPC分类号: C07D303/22 , C07D407/12
摘要: This invention relates to a method for producing a glycidyl ether of general formula (I), wherein A is an optionally substituted aryl or heteroaryl group and the asterisked carbon atom represents an asymmetric carbon atom, comprising reacting an aryl alcohol of the general formula A-OH, wherein A is as defined above, with an epihalohydrin in the presence of a quaternary ammonium salt and, if necessary, treating the reaction product with a base. This method can afford the glycidyl ether of formula (I), which is useful as an intermediate of drugs, especially a β-blocker, in a simplified manner with a high optical purity.
摘要翻译: 本发明涉及一种制备通式(I)的缩水甘油醚的方法,其中A是任选取代的芳基或杂芳基,而星号碳原子代表不对称碳原子,包括使通式为A- OH,其中A如上定义,在季铵盐存在下与表卤代醇反应,如果需要,用碱处理反应产物。 该方法可以以简单的方式提供具有高光学纯度的式(I)的缩水甘油醚,其可用作药物的中间体,特别是β-阻滞剂。
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公开(公告)号:EP0406438B1
公开(公告)日:1994-03-16
申请号:EP90900359.2
申请日:1989-12-25
申请人: KOWA COMPANY LTD.
发明人: KAWAMURA, Kiyoshi , OTA, Tomio
IPC分类号: C07D301/28
CPC分类号: C07D303/22 , C07D407/12
摘要: This invention relates to a method for producing a glycidyl ether of general formula (I), wherein A is an optionally substituted aryl or heteroaryl group and the asterisked carbon atom represents an asymmetric carbon atom, comprising reacting an aryl alcohol of the general formula A-OH, wherein A is as defined above, with an epihalohydrin in the presence of a quaternary ammonium salt and, if necessary, treating the reaction product with a base. This method can afford the glycidyl ether of formula (I), which is useful as an intermediate of drugs, especially a β-blocker, in a simplified manner with a high optical purity.
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