目的为寻找新的抗血小板聚集剂,以抗血小板聚集药物吡考他胺(picotamide)为先导化合物,对其结构进行改造,合成新的类似物。方法以苯甲醚为原料,经3步反应制得中间体4-甲氧基-1,3-苯二甲酰氯,经与不同的胺类化合物进行取代反应制得目标化合物。结果与结论共制得10个新化合物,其结构经红外和核磁共振谱确证。药理实验结果表明,化合物PN9和PN10的抗血小板聚集活性很高,明显优于阳性对照药物picotamide。 Objective To find a new anti-platelet aggregation agent, taking picotamide as an anti-platelet aggregation drug as the lead compound, its structure was modified to synthesize a new analogue. Methods Starting from anisole, the intermediate 4-methoxy-1,3-benzenedicarboxylic acid was obtained through 3 steps reaction, and the target compounds were prepared via substitution reaction with different amines. Results and Conclusion A total of 10 new compounds were prepared and their structures were confirmed by IR and 1H NMR. Pharmacological results show that compounds PN9 and PN10 anti-platelet aggregation activity is very high, significantly better than the positive control drug picotamide.