有机化学 ›› 2004, Vol. 24 ›› Issue (9): 1125-1128. 上一篇    下一篇

研究简报

新型血栓溶解剂P-6A类似物的合成研究

朱万仁*,a, 刘晓珍b, 周长军b, 雷光清b   

  1. a玉林师范学院化学与生物系 广西 537000;
    b北京药物化学研究所 北京 102205
  • 收稿日期:2004-03-18 修回日期:2004-05-27 接受日期:2004-06-18 发布日期:2022-09-20

Synthesis of New P-6A Analogues with Potent Coronary Vasodilator Effect

ZHU Wan-Ren*,a, LIU Xiao-Zhenb, ZHOU Chang-Junb, LEI Guang-Qingb   

  1. aDepartment of Chemistry and Biology, Yulin Teacher's College, Yulin 537000;
    bBeijing Institute of Pharmaceutical Chemistry, Beijing 102205
  • Received:2004-03-18 Revised:2004-05-27 Accepted:2004-06-18 Published:2022-09-20
  • Contact: * E-mail: wrzhu880@sohu.com

报道在液相中用混合酸酐法合成了新型的6个P-6A的五肽类似物.通过定向分步递进,采用反应活性较高的混合酸酐合成法,以氯甲酸异丁酯作活化剂,以THF和DMF作溶剂,使每一步合成收率均高于60%.对所合成的6个P-6A类似物进行了光学测定,元素分析和MS谱图分析确证.

关键词: 血纤维蛋白原, 溶血栓剂, P-6A类似物, 混合酸酐法, 多肽液相合成

Six new P-6A analogues were synthesized in liquid phase using THF and DMF solvents, using an active reagent of isobutyl chloroformate and mixed anhydride method in every preparation step. The yield was more than60% in every step of synthesizing peptides. Their structures were characterized by MS and elemental analysis. The examination of optical activities displayedthat the first one was right rotation and the others kept left rotation to polarized light.

Key words: fibrin mass, degraded occlusive thrombus reagent, P-6A analogue, mixed anhydride method, peptide synthesis in liquid phase