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苯并二氮杂酮酸的合成及其在肽模拟中的应用

Synthesis of Benzodiazepinonic Acid and Application in Peptide Mimetics
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摘要 采用两种方法以靛红酸酐为起始原料,分别与谷氨酸(L-Glu)和亚氨基二乙酸(Ida)反应制备两种含有游离羧基的1,4-苯并二氮杂-2,5-二酮类中间体2a和2b;同时,由2a或2b与氨基组分3c~3f,3h,3j进行缩合制备了含有1,4-苯并二氮杂-2,5-二酮环的肽模拟物4c~4f,4h,4j,5c~5f,5h,5j.另外,讨论了溶剂对微波辅助法合成1,4-苯并二氮杂-2,5-二酮酸的影响.所合成新化合物均经MS,1HNMR证明其结构. To synthesize two 1,4-benzodiazepine-2,5-dione intermediates 2a and 2b with free carboxyl, two methods were applied in this paper, in which isatoic acid was used as starting material and reacted with glutamic acid (L-Glu) and imino diacetic acid (Ida), respectively. Meanwhile, peptide mimetics 4c~4f, 4h, 4j, 5c~5f, 5h, 5j with 1,4-benzodiazepine-2,5-dione cycle were prepared by condensation of 2a or 2b with amino components 3c~3f, 3h and 3j. In addition, effect on the microwave-assisted synthesis of 1,4-benzodiazepine-2,5-dionic acid by solvent was discussed. All the new compounds were characterized by MS and 1H NMR techniques.
出处 《有机化学》 SCIE CAS CSCD 北大核心 2010年第7期1010-1016,共7页 Chinese Journal of Organic Chemistry
关键词 靛红酸酐 1 4-苯并二氮杂-2 5-二酮酸 肽模拟 微波 isatoic acid 1 4-benzodiazepine-2 5-dionic acid peptide mimetics microwave
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