呱氨托美丁的合成及活性研究

Synthesis of and activity research on amtolmetin

目的合成呱氨托美丁 ,并验证其活性。方法以托美丁为起始原料 ,在强缩水剂N ,N 羰基二咪唑的作用下 ,先生成酰胺中间产物 ,再成酯合成呱氨托美丁 ;经药理学试验 ,对其抗炎活性、镇痛作用及解热活性进行了初步研究。结果合成了目标化合物 ,药理实验结果表明 :呱氨托美丁作用与托美丁类似 ,比吲哚美辛的解热镇痛作用强。结论所采用的合成路线可行 ,呱氨托美丁具有较强的解热镇痛作用。

Aim To synthesize amtolmetin and testify its activities.Methods Tometin was used as the original material,via amidation and erterification under catalyzation of CDI to gain amotolmetin.After synthesis,pharmacologic experiments in antiflammatory activity,analgesic activity and antipyretic activity were made.Result Amtolmetin was syntesized and its activity in antiflammatory and analgesic can be compared with that of tometin and stronger than that of indomethin.Conclusion The synthetic process of amtolmetin was carried out and amtolmetin has strong antiflammatory and analgesic activities.