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鉴于4-取代苯基-1哌嗪烷醇具镇痛作用,故将其引入消炎镇痛药glafenine(1)和floctafenine(2)的分子中,使成相应的酯(3),可望由于增加脂溶性,易于吸收而增强镇痛效果。作者还以苯环替代(1)中的喹啉环制得2-(苯氨基)苯甲酸酯(4)和2-(苯氨基)烟酸酯(5),并研究了它们的构-效关系。4-苯基-1-哌嗪烷醇与2-(4喹啉氨基)苯甲酸甲酯进行酯交换可得酯(3);若与2-取代氨基苯甲酸甲酯或烟酸甲酯反应则可得酯(4)和(5)。(3)也可由4-苯基-1-哌嗪烷醇先与靛红酸醍或邻氨基苯甲酸甲酯反应,再
In view of the analgesic effect of 4-substituted phenyl-1-piperazinol, it was introduced into the molecules of the anti-inflammatory analgesics glafenine (1) and floctafenine (2) to make the corresponding esters (3) Increase fat-soluble, easy to absorb and enhance analgesic effect. The authors also prepared 2- (phenylamino) benzoate (4) and 2- (phenylamino) nicotinate (5) by replacing the quinoline ring in (1) with benzene ring and studied their structure- Effective relationship. Transesterification of 4-phenyl-1-piperazinol with methyl 2- (4quinolinamino) benzoate gives ester (3); if reacted with methyl 2-substituted aminobenzoate or methyl nicotinate Esters (4) and (5) are available. (3) can also be 4-phenyl-1-piperazine alkanol with the first 醍 or anthranilate reaction, and then