呱氨托美丁合成工艺的改进

Improved Synthesis of Amtolmetin Guacil

以托美丁钠为起始原料,与氯甲酸异丁酯、甘氨酸反应生成中间体托美丁甘氨酰胺,再与氯甲酸异丁酯、愈创木酚反应制得呱氨托美丁,同时对其的精制方法进行了研究。结果显示:改进后的工艺反应条件温和,操作简单,提高了目标物的质量,总收率65%,具有较大的产业化生产优势。

To improve the sysnthesis of amtolmetin guacil, amtolmetin guacil was synthesized using Tolmetin sodium 2 as the starting material, and with isobuty chloroformate, glycine reacted to get midbody Tolmetin glycinamide 3, then with isobuty chloroformate ,guaiacol reacted to get amtolmetin guacil 1, meanwhile researching method of refinding means of 1. Finally, reacting condition of improved technology was moderate, simplicity of oprator, improving quality of sighting vane 1 and the overall yied was 65 %, having benefit of large - scale industrialization production.