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有机化学
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有机化学 ›› 2010, Vol. 30 ›› Issue (07): 1010-1016. 上一篇    下一篇

研究论文

苯并二氮杂酮酸的合成及其在肽模拟中的应用

袁建海，杨潇骁，林浩，王德心*   

  1. (北京协和医学院 中国医学科学院药物研究所 北京 100050)
  • 收稿日期:2009-11-06 修回日期:2010-01-06 发布日期:2010-02-03
  • 通讯作者: 王德心 E-mail:wangdx@imm.ac.cn

Synthesis of Benzodiazepinonic Acid and Application in Peptide Mimetics

YUAN Jian-Hai, YANG Xiao-Xiao, LIN Hao, WANG De-Xin*     

  1. (Institute of Materia Medica, Peking Union Medical College, Chinese Academy of Medical Science, Beijing 100050)
  • Received:2009-11-06 Revised:2010-01-06 Published:2010-02-03

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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-2,5-二酮类中间体和; 同时, 由或与氨基组分～, , 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～, , , ～, , . 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, H NMR证明其结构.

关键词: 靛红酸酐, 1,4-苯并二氮杂-2,5-二酮酸, 肽模拟, 微波

To synthesize two 1,4-benzodiazepine-2,5-dione intermediates and 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 ～, , , ～, , with 1,4-benzodiazepine-2,5-dione cycle were prepared by condensation of or with amino components ～, and . 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 H NMR techniques.

Key words: isatoic acid, 1,4-benzodiazepine-2,5-dionic acid, peptide mimetics, microwave