丙谷胺的合成

Synthesis of proglumide

丙谷胺是一种抗酸药,主要用于治疗胃炎和消化性溃疡。在NaHCO3存在下,苯甲酰氯和谷氨酸钠发生反应生成苯甲酰谷氨酸。醋酸酐作为脱水剂,苯甲酰谷氨酸在60℃时反应2.5h脱水生成苯甲酰谷氨酸酐。苯甲酰谷氨酸酐与二正丙胺反应得到粗品丙谷胺,经过纯化得到了丙谷胺。丙谷胺合成的总收率为18.1%,目标产物通过红外光谱和核磁共振氢谱表征确证。该合成方法操作简单,适合工业化生产。

Proglumide is an anti-acid drug witch is widely used for the treatment of gastritis and pepticulcer.Benzoyl glutamic acid was synthesized from benzoyl chloride and monosodium glutamate in the presence of sodium bicarbonate.Benzoyl glutamic anhydride was synthesized by dehydration of the intermediates under the catalysis of acetic anhydride.Proglumide was obtained by adding dipropylamine to the above synthesized products and purification.The total yield is 18.1%.Proglumide was characterized by IR and 1 HNMR.The operation of this experiment is simple.The process is simple and suitable for industrial production.