A Novel Method for the Protection and Activation of Histidine
The yield and purity of synthetic peptides were greatly related to the amino acid protection and activation during the synthesis process.Therefore,the amino acid protection and activation are the most important steps in peptide synthesis.By using tetrahydrofuran as the solvent,9-fluorenylmethoxycarbonyl as protection group,2-(7-azobenzotri-azol-l-yl)-N,N,N,N-tetramethyluronium hexafluorophosphate (HATU) as condensation reagent an amino protected histidine ester was given.In this article a novel synthesis method for N-(9-fluorenylmethoxycarbonyl)-histidine active ester was established.The reaction conditions for preparing this active ester were optimized.The experimental results indicated that solvents and active reagents had remarkable effects on the yield of active ester.The best conditions for preparing the active ester was a ratio of n (Fmoc-His-OH)∶ n (HATU) =1∶1.2 with THF used as the solvent at room temperature.The yield of the final product was about 80% with a purity of over 85%.This simple method would provide fundamentals for the synthesis of other protected amino acid active esters.
histidine protection activation peptide
Zhao Yinan Zhang Shubiao Cui Shaohui Chen Huiying Wang Bing Zhao Yinan Zhang Shufen
Key Laboratory of Bio-chemistry Engineering-The State Ethnic Affairs Commission-Ministry of Educatio State Key Laboratory of Fine Chemicals Dalian University of Technology Dalian, China
国际会议
北京
英文
226-228
2012-10-26（万方平台首次上网日期，不代表论文的发表时间）