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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0.113mmol/L,反应时间为4min,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%.
In the thymopentin solid-phase synthesis, the introduction of microwave-assisted technology, in-depth study of the microwave under the influence of condensation reagents, solvents, reactant concentration, reaction time and temperature on the yield.Compared with the traditional method, the microwave condensation reaction The rate of increase over 15 times, multiple fold of amino acids from triple to over double the traditional reduction of thymopentin synthesis cost of about 40%; finally get pyridine / DMF as solvent, benzotriazole-N, N, N ’, N’-tetramethyluronium hexafluorophosphate as the condensation reagent, the concentration of the reaction was 0.113mmol / L, the reaction time was 4min, the reaction temperature was 20 ℃ for the best reaction conditions, when thymopentin The highest yield was 88.7%.