Department of Medicinal Chemistry School of Pharmacy, Tokyo University of Pharmacy and Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
Org Biomol Chem. 2020 Sep 23;18(36):7094-7097. doi: 10.1039/d0ob01370f.
To construct disulfide-linked hybrid molecules systematically and efficiently, we established a more practical solid-phase disulfide ligation (SPDSL) system with enhanced utility. The group Npys-OPh(pF) shows reactivity similar to that of Npys-Cl, but it is more stable. An efficient synthesis of the cyclic peptide oxytocin and a peptide-sugar conjugate was accomplished as models. These results indicate that the Npys-OPh(pF) resin functions as a common synthetic platform in SPDSL.
为了系统高效地构建二硫键连接的杂合分子,我们建立了一个更实用的固相二硫键连接(SPDSL)系统,增强了其实用性。Npys-OPh(pF) 基团显示出与 Npys-Cl 相似的反应活性,但稳定性更高。作为模型,成功合成了环状肽催产素和肽-糖缀合物。这些结果表明 Npys-OPh(pF) 树脂在 SPDSL 中可作为通用合成平台发挥作用。