Institute for Research in Biomedicine (IRB Barcelona) , The Barcelona Institute of Science and Technology , Barcelona 08028 , Spain.
CIBER-BBN, Networking Centre on Bioengineering , Biomaterials and Nanomedicine , Barcelona Science Park , Barcelona 08028 , Spain.
Org Lett. 2018 Jul 20;20(14):4306-4309. doi: 10.1021/acs.orglett.8b01741. Epub 2018 Jun 28.
Native chemical ligation (NCL) employing the N-methylbenzimidazolinone (MeNbz) linker readily provided the linear precursor of a 16-mer peptide that is difficult to obtain by stepwise solid-phase peptide synthesis. NCL and the workup conditions were improved toward a protocol that allows for quantitative removal of the 4-hydroxymercaptophenol additive and subsequent formation of the disulfide bridge in the NCL cocktail by oxidation in air, tolerated by the presence of tris(hydroxypropyl)phosphine.
采用 N-甲基苯并咪唑酮（MeNbz）连接子的天然化学连接（NCL）可以方便地提供难以通过逐步固相肽合成获得的 16 肽线性前体。NCL 和工作条件得到了改进，形成了一种方案，允许通过空气中的氧化定量去除 4-羟基巯基苯酚添加剂，并在三（羟丙基）膦存在下随后在 NCL 混合物中形成二硫键。
