微波辅助固相合成胸腺五肽的研究

在胸腺五肽的固相合成中, 引入微波辅助技术, 深入研究了微波作用下缩合试剂、溶剂、反应物浓度、反应时间和温度对产率的影响. 与传统方法相比, 微波将缩合反应速率提高了15倍以上, 氨基酸过量倍数也从传统的三倍降低到过量一倍, 减少胸腺五肽的合成成本约40%; 最终得到以吡啶/DMF为溶剂, 苯并三氮唑-N,N,N',N'-四甲基脲六氟磷酸酯为缩合试剂, 反应物浓度为0.113 mmol/L, 反应时间为4 min, 反应温度为20 ℃为最佳反应条件, 此时胸腺五肽的产率最高, 为88.7%.

Study on Microwave-Assisted Solid Phase Synthesis of Thymopentin

A microwave-irradiation technique was applied to the solid phase synthesis of thymopentin, and also the influences of coupling reagents, solvents, reactant concentration, reaction time and temperature on the solid phase synthesis yield of thymopentin with microwave irradiation were investigated. Compared with the classical method, the reaction rate of forming peptide bond was increased by over 15 times, and the excessive amount of amino acid was reduced to only one fold from 3 folds of the classical method, therefore the synthetic cost was about 40% reduced by the microwave-assisted technique. The best conditions including solvent, coupling reagent, reactant concentration, reaction time and temperature were pyridine/DMF, O-benzotriazole-N,N,N',N'-tetramethyl-uronium-hexafluorophosphate (HBTU), 0.113 mmol/L, 4 min and 20 ℃, respectively. The yield of thymopentin reached 88.7% under the best conditions.