N-甲酰-L-天冬氨酸酐的合成研究

N-甲酰-L-天冬氨酸酐是合成阿斯巴甜的中间体,为了减少副产物的生成,探索出工业生产中最佳的反应条件。以甲酸、乙酸酐和L-天冬氨酸为原料,氧化镁为催化剂,合成N-甲酰-L-天冬氨酸酐。探讨了反应温度、反应时间、甲酸、乙酸酐和催化剂的用量对反应收率和产物熔点的影响。结果表明,最佳的反应条件为:反应温度50℃,反应时间5 h,物质的量比n(氧化镁)∶n(甲酸)∶n(乙酸酐)∶n(L-天冬氨酸)=0.01∶1.2∶2.5∶1.0,此时产物的纯度较好,收率为85.5%。

Study on Synthesis of N - Formyl - L - Aspartic Anhydride

N - formyl - L - aspartic anhydride was a synthetic intermediate of aspartame, in order to reduce the generation of by - products and explore the industrial production in optimal conditions, N - Formyi - L - aspartic anhydride was synthesized with magnesium oxide catalyst in formic acid and acetic anhydride solvent. The effects of temperature, reaction times, molar ratio of formic acid, acetic anhydride and catalyst on the reaction yield and the melting point of the product were discussed. The results showed that the optimum reaction conditions were temperature 50 ℃, reaction time 5 h, and the molar ratio of magnesium oxide ： formic acid ： acetic anhydride ： L - aspartic acid = 0. 01 ： 1.2 ： 2.5 ： 1.0. The purity of the product was preferable, and the yield was 85.5%.