使用新型耦合活化剂Oxyma高效合成利拉鲁肽
收稿日期: 2015-05-08
修回日期: 2015-08-03
网络出版日期: 2015-09-06
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
Received date: 2015-05-08
Revised date: 2015-08-03
Online published: 2015-09-06
Supported by
Project supported by the National Natural Science Foundation of China (Nos. 21272223, 21572214).
王风亮 , 许玲 , 储国超 , 石景 , 郭庆祥 . 使用新型耦合活化剂Oxyma高效合成利拉鲁肽[J]. 有机化学, 2016 , 36(1) : 218 -221 . DOI: 10.6023/cjoc201505014
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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