ω-芋螺毒素线性肽合成方法比较

Comparison of synthetic methods of several ω-conotoxins linear peptides

比较了不同偶合方法及裂解条件对ω 芋螺毒素及其衍生物线性肽合成效率的影响。结果表明 ,Boc Bzl策略、Fmoc But策略、手工及仪器对总偶合率影响较小 ,但裂解条件及保护策略对肽 树脂裂解影响很大 ,氟化氢体系裂解Boc Bzl法合成树脂副产物较多 ,且主链易发生断裂 ,以低高法裂解效率最高。三氟乙酸体系裂解Fmoc法合成树脂效率高 ,主要副产物是含Trt基的线性肽 ,增加1,2

Effects of coupling methods and cleavage conditions on synthetic efficiency of several ω?conotoxins were studied. The results showed that manual or automatic Boc/Bzl and Fmoc/But synthetic method had little effect on the efficiency of coupling, but cleavage conditions had great effects. HF cleavage method could bring on more vice?product than TFA method, and linear chain was cleaved partially, 'low?high' HF cleavage have more advantage than 'High' method. The main vice?product of TFA cleavage was linear peptide which Trt protecting groups were not removed completely, increment of 1,2?ethanedithiol could inhibit these vice?reaction.