Fmoc法固相合成胸腺五肽工艺

Solid-Phase Synthesis of Thymopentin Using Fmoc-Based Strategy

采用Fmoc法固相合成胸腺五肽(TP-5)。利用RP-HPLC和质谱对其进行鉴定,绘制胸腺五肽纯品的标准曲线,作为胸腺五肽的准确定量方法。考察不同的反应溶剂、缩合剂和切割条件对合成胸腺五肽纯度的影响,并由此确定最佳合成工艺条件:以DMF为反应溶剂,HATU为缩合剂,TFA、p-甲基苯酚、EDT和H2O体积比为97.00∶0.25∶0.25∶2.50溶液为切割条件。在此条件下,胸腺五肽的纯度达到80.34%。

Thymopentin （TP-5） has been synthesized by solid-phase method, and determined by reversedphase high performance liquid chromatography and mass spectrum. The standard curve of TP-5 has been drawn, and used as a method to exactly analyze the purity of crude TP-5. The influence of different coupling solvents, coupling reagents and cleavage conditions on the purity of TP-5 is reviewed. The optimized protocol is ascertained：DMF is used as the coupling solvent;HATU as the coupling reagent;and TFA：p-methyl phenol： EDT： H2O = 97 ： 0. 25 ： 0.25 ： 2.5 as the cleavage condition. Under this condition, the final purity of crude TP-5 reached 80.34 % .