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

作　　者：袁建海[1] 杨潇骁[1] 林浩[1] 王德心[1] 

机构地区：[1]f北京协和医学院中国医学科学院药物研究所,北京100050

出　　处：《有机化学》2010年第7期1010-1016,共7页Chinese Journal of Organic Chemistry

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.

关 键 词：靛红酸酐 1 4-苯并二氮杂-2 5-二酮酸 肽模拟 微波 

分 类 号：TQ460.1[化学工程—制药化工]