Yano Shinya, Mori Toshihiro, Kubota Hideki
Iwate Drug Synthesis R&D Center, Sekisui Medical Co., Ltd., Iwate 028-7305, Japan.
Molecules. 2021 Jun 8;26(12):3497. doi: 10.3390/molecules26123497.
Addition of the silylated tag (STag) enables peptides to be highly soluble in CPME, allowing them to be used at high concentrations in a coupling reaction to enhance reactivity and achieve effective synthesis of sterically hindered peptides. We described the development of a continuous one-pot STag-assisted peptide synthesis platform as a method that provides near-stoichiometric, speedy, environmentally friendly, and scalable peptide synthesis.
添加硅烷化标签(STag)可使肽在环戊基甲基醚(CPME)中具有高度溶解性,从而能够在偶联反应中以高浓度使用,以增强反应活性并实现空间位阻肽的有效合成。我们描述了一种连续一锅法STag辅助肽合成平台的开发,该方法可提供接近化学计量比、快速、环保且可扩展的肽合成。