Methods for preparing 5-aroyl-1,2-dihydro-3h-pyrrolo-(1,2-a)Pyrrole-1-carboxylic acids
申请人:Ohmeda Pharmaceutical Products Division Inc.
公开号:EP0791595A1
公开(公告)日:1997-08-27
This invention pertains to methods for preparing 5-aroyl-1,2-dihydro-3H-pyrrolo-[1,2-a]pyrrole-1-carboxylic acids represented by formula (I):
The acids have useful analgesic, anti flammatory and antipyretic properties.
In a first embodiment, the method comprises the sequential steps of cyclizing, via a free radical ring closure reaction, and hydrolyzing a compound represented by formula (IV):
wherein R1 is lower alkyl containing from 1-4 carbon atoms.
In a second embodiment, the method comprises the sequential steps of hydrolyzing and decarboxylating a compound represented by formula (VIII):
本发明涉及制备式(I)代表的 5-芳酰基-1,2-二氢-3H-吡咯并[1,2-a]吡咯-1-羧酸的方法:
这些酸具有有效的镇痛、抗炎和解热特性。
在第一个实施方案中,该方法包括通过自由基闭环反应使式(IV)代表的化合物环化和水解的连续步骤:
其中 R1 是含有 1-4 个碳原子的低级烷基。
在第二个实施方案中,该方法包括对式(VIII)代表的化合物进行水解和脱羧的连续步骤: