自组装多功能反应器固相合成依非巴特

Solid-phase Synthesis of Eptifibatide in a Multifunctional Reactor

采用集反应、搅拌、鼓泡、N2气保护和过滤五重功能的自组装反应器,研究了树脂种类、溶剂、缩合试剂和反应时间对环肽依非巴特产率的影响。结果表明,以Rink Amide AM树脂为固相载体,HBTU/HOBt/DIEA为肽键缩合剂,DMF为溶剂,反应2 h,粗肽得率高达86.6%,经液相色谱纯化后纯度达98%以上。

A home-made reactor possessing functions including reaction, blending, bubbling, protecting with N2 and filtration was fabricated. The effects of the type of resin, solvent, coupling reagent and reaction time on the yield of cyclic eptifibatide were investigated. The results showed the overall yield was up to 86. 6%, using Rink Amide AM resin as solid supporter, HBTU/HOBt/DIEA as the coupling reagent, DMF as the solvent and reaction 2 hours in the reactor. The purity of the product as revealed by HPLC could reach 98%.