Fmoc法固相合成胸腺五肽工艺

摘要采用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%。

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	张成刚
	甘一如
	黄鹤

关键词：胸腺五肽固相合成 RP-HPLC 标准曲线

Abstract： Thymopentin(TP-5) has been synthesized by solid-phase method,and determined by reversed-phase 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∶H_2O=97∶0.25∶0.25∶2.5 as the cleavage condition.Under this condition,the final purity of crude TP-5 reached 80.34%.

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Received 2005-11-15; published 2005-11-15

引用本文:

张成刚,甘一如,黄鹤.Fmoc法固相合成胸腺五肽工艺[J]. 化学工业与工程, 2005,22(6): 407-410

ZHANG Cheng-gang,GAN Yi-ru,HUANG He.Solid-Phase Synthesis of Thymopentin Using Fmoc-Based Strategy[J]. Chemcial Industry and Engineering, 2005,22(6): 407-410

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