Chin. J. Org. Chem. ›› 2016, Vol. 36 ›› Issue (1): 218-221.DOI: 10.6023/cjoc201505014 Previous Articles     Next Articles



王风亮, 许玲, 储国超, 石景, 郭庆祥   

  1. 中国科学技术大学化学系 合肥 230026
  • 收稿日期:2015-05-08 修回日期:2015-08-03 发布日期:2015-09-06
  • 通讯作者: 石景, 郭庆祥;
  • 基金资助:

    国家自然科学基金(Nos. 21272223, 21572214)资助项目.

Efficient Synthesis of Liraglutide by Using Oxyma as Coupling Reagent

Wang Fengliang, Xu Ling, Chu Guochao, Shi Jing, Guo Qingxiang   

  1. Department of Chemistry, University of Science and Technology of China, Hefei 230026
  • Received:2015-05-08 Revised:2015-08-03 Published:2015-09-06
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 21272223, 21572214).

As a newly efficient reagent, Oxyma [ethyl 2-cyano-2-(hydroxyimino)acetate] has a lower rate of racemization and relative higher coupling efficiency as compared with HOBt, HOAt, etc. In this work, as an important polypeptide drug for the treatment of diabetes, liraglutide was firstly chemically synthesized with high efficiency by solid chemical synthesis using Oxyma as coupling reagent. The strategy presented here provides an efficient strategy for the chemical synthesis of liraglutide with enlarged scales.

Key words: oxyma, liraglutide, polypeptide drug, solid poly-peptide synthesis