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Synthesis of Diethyl N-{4-[N-Methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]-benzoyl}-L-glutamate and Its Derivatives
Deng Xiling1,3; Liu Weidong1; Li Chao1; Zhang Zhili1; Wang Xiaowei1; Liu Junyi1,2
关键词5-(Substituted)Amino Pyrimidine New Anticancer Agent Synthesis
刊名CHINESE JOURNAL OF ORGANIC CHEMISTRY
2011
31期:1页:75-81
收录类别SCI
文章类型Article
WOS标题词Science & Technology
类目[WOS]Chemistry, Organic
研究领域[WOS]Chemistry
关键词[WOS]ANTIFOLATE
英文摘要

A new practical approach to prepare diethyl N-{4-[N-methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]benzoyl}-L-glutamate and its derivatives has been realized from ethyl 4-aminobenzoate (4a) and diethyl N-(4-aminobenzoyl)-L-glutamate (4b). Six novel 5-(substituted)amino pyrimidines 9 similar to 11 were synthesized via methylation, allylation, bromohydroxylation, epoxidation, ring-opening, deprotection reaction and so on, and were characterized by (1)H NMR, (13)C NMR and MS techniques. The inhibitory activities against human dihydrofolate reductase of the compounds have been determined. The results showed that the bioactivities of the compounds were related with L-glutamate side chain.

语种中文
WOS记录号WOS:000287782400008
引用统计
被引频次:1[WOS]   [WOS记录]     [WOS相关记录]
文献类型期刊论文
条目标识符http://ir.bjmu.edu.cn/handle/400002259/50526
专题北京大学药学院_化学生物学系
作者单位1.Peking Univ, Sch Pharmaceut Sci, Dept Biol Chem, Beijing 100191, Peoples R China
2.Peking Univ, State Key Lab Nat & Biomimet Drug, Beijing 100191, Peoples R China
3.Shihezi Univ, Sch Pharmaceut Sci, Dept Pharmaceut Sci, Shihezi 832002, Peoples R China
推荐引用方式
GB/T 7714
Deng Xiling,Liu Weidong,Li Chao,et al. Synthesis of Diethyl N-{4-[N-Methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]-benzoyl}-L-glutamate and Its Derivatives[J]. CHINESE JOURNAL OF ORGANIC CHEMISTRY,2011,31(1):75-81.
APA Deng Xiling,Liu Weidong,Li Chao,Zhang Zhili,Wang Xiaowei,&Liu Junyi.(2011).Synthesis of Diethyl N-{4-[N-Methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]-benzoyl}-L-glutamate and Its Derivatives.CHINESE JOURNAL OF ORGANIC CHEMISTRY,31(1),75-81.
MLA Deng Xiling,et al."Synthesis of Diethyl N-{4-[N-Methyl-N-(3-(2,4-dioxo-1,2,3,4-tetrahydropyrimidin-5-yl)amino-2-hydroxypropyl)amino]-benzoyl}-L-glutamate and Its Derivatives".CHINESE JOURNAL OF ORGANIC CHEMISTRY 31.1(2011):75-81.
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