| 对甲氨基苯甲酰谷氨酸二乙酯的合成方法 |
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| 引用本文： | 田超,周受辛,王彪,邓喜玲,郭莹,张志丽,王孝伟,刘俊义. 对甲氨基苯甲酰谷氨酸二乙酯的合成方法[J]. 北京大学学报(医学版), 2008, 40(4): 443-445 |
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| 作者姓名： | 田超 周受辛 王彪 邓喜玲 郭莹 张志丽 王孝伟 刘俊义 |
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| 作者单位： | (1.北京大学药学院化学生物学系,北京 100083;2.天然药物及仿生药物国家重点实验室) |
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| 摘 要： | 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广谷氨酸二乙酯(1).结果:合成目标化合物只需2步反应,反应时间仅6 h,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.
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| 关 键 词： | L-谷氨酸二乙酯衍生物 伯胺 N-单甲基化 N-苄基化 |
Synthesis of Diethyl N-[p-(Methylamino)benzoyl]-L-glutamate |
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| TIAN Chao,ZHOU Shou-xin,WANG Biao,DENG Xi-ling,GUO Ying,ZHANG Zhi-li,WANG Xiao-wei,LIU Jun-yi. Synthesis of Diethyl N-[p-(Methylamino)benzoyl]-L-glutamate[J]. Journal of Peking University. Health sciences, 2008, 40(4): 443-445 |
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| Authors: | TIAN Chao ZHOU Shou-xin WANG Biao DENG Xi-ling GUO Ying ZHANG Zhi-li WANG Xiao-wei LIU Jun-yi |
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| Affiliation: | Department of Chemical Biology, Peking University School of Pharmaceutical Sciences, Beijing 100083, China. |
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| Abstract: | 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-(methylamino)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-(methylamino)benzoyl]-L-glutamate. |
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| Keywords: | L-glutamate diethylester derivatives Primary amine N-monomethylation N-benzylation |
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