采用控温微波加热直接固相合成β-淀粉样肽（1-42）。

Direct solid-phase synthesis of the beta-amyloid (1-42) peptide using controlled microwave heating.

机构信息

Christian Doppler Laboratory for Microwave Chemistry and Institute of Chemistry, Karl-Franzens-University Graz, Heinrichstrasse 28, A-8010 Graz, Austria.

出版信息

J Org Chem. 2010 Mar 19;75(6):2103-6. doi: 10.1021/jo100136r.

DOI:10.1021/jo100136r

PMID:20180552

Abstract

Standard linear Fmoc/t-Bu solid-phase synthesis of the 42-mer beta-amyloid (1-42) peptide was achieved under controlled microwave conditions at 86 degrees C using inexpensive DIC/HOBt as coupling reagent on ChemMatrix resin. In order to avoid racemization of the sensitive amino acids, the coupling of the three His residues in the difficult peptide sequence was performed at room temperature. The desired peptide was obtained within 15 h overall processing time in high yield and purity (78% crude yield).

摘要

在 86°C 微波条件下，使用廉价的 DIC/HOBt 作为偶联试剂，在 ChemMatrix 树脂上，通过标准线性 Fmoc/t-Bu 固相合成方法，成功合成了 42 肽β-淀粉样蛋白（1-42）。为了避免敏感氨基酸的外消旋化，在室温下对困难肽序列中的三个 His 残基进行了偶联。在 15 小时的总处理时间内，以高收率和高纯度（78%粗产物收率）得到了所需的肽。