维格列汀合成工艺研究

Study on the Synthesis of Vildagliptin

目的优化维格列汀的合成工艺。方法以L-脯氨酰胺与氯乙酰氯为原料通过酰氨化、脱水反应制得的关键中间体再与3-氨基-1-金刚烷醇通过缩合反应制得目标产物。结果目标产物经过质谱和核磁共振氢谱以及碳谱确认化学结构,总收率为60%,纯度为99.9%。结论所得合成工艺操作简便,反应条件较为温和,产品纯度和收率较高,适合工业化生产。

OBJECTIVE To optimize the synthesized of vildagliptin. METHODS The key intermediate was synthesized by using L-prolinamide and chloroacetyl chloride as raw materials through amidation and dehydration,then vildagliptin was synthesized by using the intermediate and 3-amino-1-adamantanol as raw materials through condensation reaction. RESULTS Vildagliptin was characterized by MS, 1H-NMR and 13 C-NMR,the total yield was 60% and the purity was 99.9%. CONCLUSION The synthetic process of vildagliptin with simple operation,mild conditions,high yield,high purity and suitable for industrial production was provided.