申请人:Dainippon Ink and Chemicals, Inc.
公开号:US06271416B1
公开(公告)日:2001-08-07
The present invention relates to a simple method for preparing a quinolinone derivative, which is effective as a medicine, e.g., as an agent for treating allergic diseases and the like; novel amide derivatives effective as an intermediate in the method, novel quinolinone derivatives obtained according to the method; and an anti-allergic agent containing a quinolinone derivative and/or physiological salt of the same as the active ingredients. The quinolinone derivative is expressed by the following general formula (II); and the method is characterized in that an amide derivative, expressed by the following general formula (I), is reacted with a basic agent, followed by intramolecular ring formation:
General Formula (I)
[wherein, R1 represents a hydrogen atom, an alkyl group, an alkyl group containing a hydroxyl group, an alkenyl group, or an aryl group; R2 represents an alkyl group, an alkenyl group, an aryl group, or an aralkyl group; R3 represents a reactive carboxyl group; and R4 to R7 represent, respectively and independently, a hydrogen atom, a hydroxyl group, an alkyl group, an alkoxy group, an alkenyl group, an alkenyloxy group, an aryl group, an aryloxy group, an aralkyloxy group, a R8R9N group (wherein, R8 and R9 represent, respectively and independently, a hydrogen atom, an alkyl group, an alkenyl group, an aralkyl group, or an acyl group), a nitro group, or a R10OOC group (wherein, R10 represents a hydrogen atom, an alkyl group, an alkenyl group, an aryl group, or an aralkyl group)].
General Formula (II)
[wherein, R1, R2 and R4 to R7 represent, respectively, the same constituents as described in general formula (I)].
本发明涉及一种简单的制备喹诺酮衍生物的方法,该方法可作为药物,例如用作治疗过敏性疾病等的药剂;在该方法中作为中间体的新型酰胺衍生物,根据该方法获得的新型喹诺酮衍生物;以及含有喹诺酮衍生物和/或其生理盐作为活性成分的抗过敏剂。喹诺酮衍生物由以下通式(II)表示;该方法的特点在于,将由以下通式(I)表示的酰胺衍生物与碱性试剂反应,然后进行分子内环形成:通式(I)中,R1表示氢原子、烷基、含有羟基的烷基、烯基或芳基;R2表示烷基、烯基、芳基或芳基烷基;R3表示反应性羧基;R4至R7分别且独立地表示氢原子、羟基、烷基、烷氧基、烯基、烯氧基、芳基、芳氧基、芳基烷氧基、R8R9N基(其中,R8和R9分别且独立地表示氢原子、烷基、烯基、芳基烷基或酰基)、硝基或R10OOC基(其中,R10表示氢原子、烷基、烯基、芳基或芳基烷基);通式(II)中,R1、R2和R4至R7分别表示与通式(I)中描述的相同成分。