目的:寻找一条合成N-[4-(甲氨基)苯甲酰基]-L-谷氨酸二乙酯的最佳方法。方法:以对氨基苯甲酰谷氨酸二乙酯(2)为起始物,经苄基化、甲基化组合成的"一锅"反应,高产率地制备了N-[4-(N-苄基-N-甲氨基)苯甲酰基]-L-谷氨酸二乙酯(3),化合物3经Pd/C催化氢化脱苄基,得到了目标化合物N-[4-(甲氨基)苯甲酰基]-L-谷氨酸二乙酯(1)。结果:合成目标化合物只需2步反应,反应时间仅6h,总产率达到88%,目标化合物通过1HNMR和MS鉴定结构正确。结论:利用上述方法可以方便高效地制备N-[4-(甲氨基)苯甲酰基]-L-谷氨酸二乙酯。
Objective :To find a best synthesis method of diethyl N-[p-(methylamino) benzoyl ]-L-glutamate(1). Methods: Using diethyl N-(p-aminobenzoyl)-L-glutamate (2) as a starting material via a one-pot process of benzylation and methylation, the diethyl N- [ p- ( methyl amino) benzoyl ] -L-glutamate (3) is prepared in high yield. Then compound 1 was conveniently obtained from debenzylation of compound 3 by Pd/C. Results: The target compound was obtained through 2-step reaction in 88% overall yield in only 6 h, and its structure was identified by ^1 HNMR and MS. Conclusion: It is a convenient and efficient method of preparation of diethyl N-[p-( methyl amino)benzoyl ]-L-glutamate.