Chin. J. Org. Chem. ›› 2008, Vol. 28 ›› Issue (05): 851-856. Previous Articles     Next Articles

Original Articles

微波作用下的多肽固相缩合反应及动力学研究

杨明,王卫国,李佩华,张俊,沈树宝*   

  1. (南京工业大学制药与生命科学学院 南京 210009)
  • 收稿日期:2007-03-30 修回日期:2007-10-20 发布日期:2008-05-20
  • 通讯作者: 沈树宝

Solid Phase Peptide Coupling and Its Kinetics under Microwave Irradiation

YANG Ming,WANG Wei-Guo,LI Pei-Hua,ZHANG Jun,SHEN Shu-Bao*   

  1. (College of Life Science and Pharmacy, Nanjing University of Technology, Nanjing 210009)
  • Received:2007-03-30 Revised:2007-10-20 Published:2008-05-20
  • Contact: SHEN Shu-Bao

The coupling of Fmoc-Val-OH to NH2-Tyr(t-Bu)-Wang resin and its kinetics were studied under microwave irradiation and conventional heating. The effect of reaction temperature on reaction rate was determined and the macroscopic kinetic parameters were obtained. The reaction stage is 2.3 and the activation energy is 104.7 kJ/mol under 300 W microwave irradiation, while the reaction stage is 2.9 and the activation energy is 142.4 kJ/mol under normal heating. The microwave irradiation brought the coupling yield of 68% under conventional heating up to 95% and the time required was shorten to 1/14 of that in conventional method.

Key words: solid phase peptide synthesis, coupling reaction, action kinetics, microwave synthesis