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有机化学
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有机化学 ›› 2006, Vol. 26 ›› Issue (06): 826-830. 上一篇    下一篇

研究论文

微波辅助固相合成胸腺五肽的研究

王卫国，李佩华，沈树宝*，应汉杰，欧阳平凯   

  1. (南京工业大学国家生化工程技术研究中心 南京 210009)
  • 收稿日期:2005-08-04 修回日期:2005-12-21 发布日期:2006-05-31
  • 通讯作者: 沈树宝

Study on Microwave-Assisted Solid Phase Synthesis of Thymopen-tin

WANG Wei-Guo,LI Pei-Hua,SHEN Shu-Bao*,YING Han-Jie
OUYANG Ping-Kai   

  1. (National Engineering Research Centre for Biochemistry, Nanjing University of Technology, Nanjing 210009)
  • Received:2005-08-04 Revised:2005-12-21 Published:2006-05-31
  • Contact: SHEN Shu-Bao

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1131

被引次数

34 | 11

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%.

关键词: 胸腺五肽, 固相合成, 溶剂, 温度, 微波

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.

Key words: thymopentin, temperature, solid phase synthesis, solvent, microwave