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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.
Oxyma, as an important new type of coupling activator, has many advantages such as lower racemization rate and higher coupling efficiency compared with HOBt, HOAt and other traditional activators.In this study, Oxyma was used as a coupling activator in the resin Liraglutide, a peptide drug with diabetes mellitus, was synthesized on a one-time basis and has high synthetic efficiency. The use of this strategy has made it possible to synthesize Liraglutide on a large scale using chemical methods.