Chin. J. Org. Chem. ›› 2010, Vol. 30 ›› Issue (07): 1010-1016. Previous Articles     Next Articles

Full Papers

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

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