Efficient Synthesis of Liraglutide by Using Oxyma as Coupling Reagent

doi:10.6023/cjoc201505014

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

Notes

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

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 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

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).

1. Efficient Synthesis of Liraglutide by Using Oxyma as Coupling Reagent.PDF(189KB)

Abstract

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

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Wang Fengliang, Xu Ling, Chu Guochao, Shi Jing, Guo Qingxiang. Efficient Synthesis of Liraglutide by Using Oxyma as Coupling Reagent[J]. Chin. J. Org. Chem., 2016, 36(1): 218-221.

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使用新型耦合活化剂Oxyma高效合成利拉鲁肽

Efficient Synthesis of Liraglutide by Using Oxyma as Coupling Reagent

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