Direct Solid-Phase Synthesis of the β-Amyloid (1-42) Peptide Using Controlled Microwave Heating
Direct Solid-Phase Synthesis of the β-Amyloid (1-42) Peptide Using Controlled Microwave Heating
复制标题
DOI：
10.1021/jo100136r
复制
发表时间：
2010-03-19
影响因子：
3.6
通讯作者：
Kappe, C. Oliver
中科院分区：
文献类型：
--
作者：
Bacsa, Bernadett;Bosze, Szilvia;Kappe, C. Oliver
以廉价的DIC/HOBt为偶联剂，在化学基质树脂上，在86℃的可控微波条件下，实现了42聚体β-淀粉样多肽的标准线性Fmoc/t-Bu固相合成。为了避免敏感氨基酸的外消旋，在室温下对难处理的多肽序列中的三个His残基进行偶联。在15h内得到所需的多肽，产率和纯度均较高(粗得率为78%)。
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).