依帕司他的合成工艺改进

Improved method of epalrestat synthesis

目的 :合成依帕司他 ,并对合成工艺进行适当改进。方法 :以甘氨酸、二硫化碳和氯乙酸钠为原料反应制得 3-羧甲基若丹宁 ,以苯甲醛和丙醛反应制得 α-甲基肉桂酸 ,最后用浓氨水将二者进行缩合 ,得到依帕司他。结果 :利用上述合成方法 ,成功制得目标化合物 ,总收率达 6 0 .7%。结论 :该合成工艺不仅原料易得 ,操作简单 ,而且总收率高 ,是适合工业化生产依帕司他的良好工艺。

Objective: To synthesize epalrestat and to improve the method of synthesis. Methods:Glycine reac-ted with carbondisulfide,then with ClCH 2COONa to give 3-carboxymethylrhodanine.PhCHO reacted with CH 3CH 2CHO in NaOH/EtOH solution to produce 2-methylcinnamaldehyde.3-carboxymethylrhodanine and 2-methylcinnamaldehyde were treated with NH 3·H 2O to obtain epalrestat. Results: The described method was effective in synthesis of Epalrestat and the yield was higher than that of in references. Conclusion: The results suggest that this method is suitable for industrial production.