固相多肽合成中N-甲基氮杂丙氨酸引入方法的建立
首发时间:2019-03-05
摘要:本文利用液相合成的小分子通过有效的一个偶联反应实现了氮杂丙氨酸的快速引入,后续通过简便的Fmoc脱除后就可实现肽链在固相上的延伸,多肽链偶联完成后可通过一步mistunobu反应来对氮杂丙氨酸的β位N进行甲基化修饰,实现了氮杂多肽的快速合成与修饰目的。
关键词: 氮杂丙氨酸 固相合成 mistunobu反应 甲基化
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Establishment of methods about the introduction of N-methyl-Aza-alanine based on solid phase peptide synthesis
Abstract:In this paper, the rapid introduction of aza-alanine was successfully achieved by an effective coupling reaction using small molecules synthesized in liquid phase. The enlongation of the peptide chain on the solid phase then can be simplely achieved upon Fmoc removal. When the coupling of the peptide chain is completed, it can be passed through a step of mistunobu reaction which is to alkylate the β-position of aza-alanine to achieve rapid synthesis and modification of the aza-peptide.
Keywords: Aza-alanine Solid Phase Synthesis Mistunobu reaction Methylation
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