Chin. J. Org. Chem. ›› 2005, Vol. 25 ›› Issue (06): 712-715. Previous Articles     Next Articles

Original Articles

赖氨酸衍生氮杂大环化合物的固相合成

杨潇骁,邱传亮,王德心*   

  1. (中国医学科学院药物研究所 北京 100050)
  • 收稿日期:2004-06-25 修回日期:2004-01-04 发布日期:2005-05-30
  • 通讯作者: 王德心

Solid-phase Synthesis of Aza-macrocyclic Compounds Derived from Lysine Residues

YANG Xiao-Xiao, QIU Chuan-Liang, WANG De-Xin*   

  1. (Institute of Materia Medica, Chinese Academy of Medical Science, Beijing 100050)
  • Received:2004-06-25 Revised:2004-01-04 Published:2005-05-30
  • Contact: WANG De-Xin

Triaza-macrocyclic compounds, based on the pseudo-dilution effect on solid support, were designed and synthesized. The key building blocks for cyclization were two lysine residues and bromoacetic acid as the bridging components via acylation-SN2 reaction in sequence. By present procedure, five target compounds 8, 9, 10, 12 and 13 with trinitrogen atoms in a 16-membered ring were obtained in good overall yields of 68.9%~86.1% and characterized by amino acid analysis and ESI-MS.

Key words: nitrogen containing macro-ring, peptide structure modification, solid-phase synthesis