活性三肽法氏囊素的液相合成  

Liquid Phase Synthesis of the Bioactive Tripeptide Bursin

作　　者：刘国都[1] 周乐[1] 

机构地区：[1]西北农林科技大学生命科学学院,陕西杨凌712100

出　　处：《西北农业学报》2008年第1期46-49,57,共5页Acta Agriculturae Boreali-occidentalis Sinica

基　　金：国家自然科学基金资助项目(30571042);杨凌农业科技开发基金资助项目(2004JA22)

摘　　要：以保护性氨基酸Boc-Lys-(Boc)-OH、Fmoc-His-(Trt)-OH和Gly-NH2-HCl为原料,N,N’-二环己基碳二亚胺(DCC)为缩合剂,按照由C端向N端依次接肽的合成策略,采用液相法完成了法氏囊素(L-Lys-His-Gly-NH2)的合成,总产率≥62.7%,其纯度≥90%。对DCC缩合反应中,羧基的活化、反应溶剂的选择、反应物投料比及顺序、反应温度及时间对反应结果的影响以及Boc、Fmoc、Trt三种保护基团的脱除条件也进行了研究和优化。The bioactive tripeptide-bursin （L-Lys-His-Gly-NH2） was synthesized from carboxy-termihal to amino-terminal in the liquid phase by the coupling reagent dicyclohexylcarbodiimide, with Boc- Lys-（Boc）-OH,Fmoc-His-（Trt）-OH,Gly-NH2-HCl as the raw materials which were all protected amino acids,the yield was not less than 62.7% for Fmoc-His-（Trt）-OH, the purity was not less than 90%. The effect of carboxylic activation, selection of solvents in the reaction, mole ratio of reactants, temperature and time in the coupling reaction and the selection of the removal condition of the three protective group Boc-, Fmoc-, Trt- was all discussed and optimized in this paper.

关 键 词：活性三肽 法氏囊素 碳二亚胺法(DCC法) 液相合成 L-Lys-His-Gly-NH2 

分 类 号：Q51[生物学—生物化学]