有机化学 ›› 2016, Vol. 36 ›› Issue (1): 218-221.DOI: 10.6023/cjoc201505014 上一篇    下一篇

研究简报

使用新型耦合活化剂Oxyma高效合成利拉鲁肽

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 出版日期:2016-01-25 发布日期:2015-09-06
  • 通讯作者: 石景, 郭庆祥 E-mail:shijing@ustc.edu.cn;qxguo@ustc.edu.cn
  • 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 Online:2016-01-25 Published:2015-09-06
  • Supported by:

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

Oxyma作为一种重要的新型耦合活化剂, 相比于HOBt, HOAt等传统活化剂具有在多肽偶联反应中消旋率较低及耦合效率更高等优势. 本研究使用Oxyma作为耦合活化剂在树脂上一次性合成了具有治疗糖尿病功能的多肽药物利拉鲁肽(Liraglutide), 且具有较高的合成效率. 该策略的运用为使用化学方法大规模合成Liraglutide提供了可能.

关键词: Oxyma, 利拉鲁肽, 多肽药物, 多肽固相合成

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