申请人:DAINIPPON INK AND CHEMICALS, INC.
公开号:EP0927718A1
公开(公告)日:1999-07-07
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 contaiirng 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 aikenyl 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)].
本发明涉及一种制备喹啉酮衍生物的简便方法,该衍生物可有效地用作药物,如治疗过敏性疾病等的药物;在该方法中作为中间体有效的新型酰胺衍生物;根据该方法获得的新型喹啉酮衍生物;以及含有喹啉酮衍生物和/或其生理盐作为有效成分的抗过敏药物。喹啉酮衍生物由以下通式(II)表示;该方法的特征在于,由以下通式(I)表示的酰胺衍生物与碱性剂反应,然后进行分子内成环:
通式 (I)
[其中,R1 代表氢原子、烷基、含羟基的烷基、烯基或芳基;R2 代表烷基、烯基、芳基或芳烷基;R3 代表活性羧基;以及 R4 至 R7 分别独立地代表氢原子、羟基、烷基、烷氧基、烯基、烯氧基、芳基、芳氧基、芳烷氧基、R8R9N 基团(其中,R8 和 R9 分别独立地代表氢原子、羟基、烷基、烷氧基、烯基、烯氧基、芳氧基、芳烷氧基、芳烷氧基)、分别独立地代表氢原子、烷基、烯基、芳基或酰基)、硝基或 R10OOC 基团(其中,R10 代表氢原子、烷基、烯基、芳基或芳基)]。
通式 (II)
[其中,R1、R2 和 R4 至 R7 分别代表与通式 (I) 所述相同的成分]。