酸敏性PEG载体的合成及其在多肽合成中的应用

本文通过聚苯乙烯固载聚乙二醇氨基树脂与羟甲基苯氧乙酸缩合制备了具有酸敏手臂结构的对羟甲基苯氧乙酰胺ＰＥＧ树脂。在合成中改进了ＰＳ－ＰＥＧＮＨ２树脂的制备方法，提高了树脂上功能基的转化率，不必进行封闭剩余活性基的操作，就得到具有单一功能基的树脂。

SYNTHESIS AND APPLICATION OF A NEW ACID-LABILE POLYETHYLENE GLYCOL RESIN FOR SOLID PHASE PEPTIDE SYNTHESIS

PEG resins with acid-labile linkage, 4-hydroxymethylphenoxyacetamide were prepared by condensation of PS-PEG-NH2 and 4-hydroxymethylpheoxy acetic acid in the presence of HOBt/CC. This PS-PEG-HMPA resin derivative was applied as a solid support for the stepwise synthesis of peptide fragment of albumin KQTALYYC according to the Fmoc solid chase synthesis strategy. The coupling and the deprotection steps in peptide synthesis proceeded in nearly quantitative yields. The peptidyl-resin was cleaved by 95% TFA. The crude peptide was purified by C18 FLC and HPLC. Analysis showed that the peptide contains expected amino acid composition. The experimental results showed that condensation reaction on the PS-PEG-AMPA proceed faster than that on acid-sensitive PS resin.