This study describes a methodological advancement in solution-phase peptide synthesis via the development of a convenient and operational protocol to synthesize oligopeptides in a one-pot three-step cascade method, in which two peptide bonds are introduced chemoselectively. Tri- to hexapeptides were obtained in high global yields (80–95%) with virtually no epimerization as determined via HPLC. The methodology described herein represents a faster, easier and milder approach to the synthesis of peptides, and it operates at equimolar amounts. This protocol comprises the formation of secondary and tertiary amides and is compatible with Z, Boc and Fmoc N-protecting groups as well as the use of D/L and non-proteinogenic amino acids.

中文翻译：

---

通过双化学选择性偶联高效地一锅法组装肽

这项研究描述了通过开发一种方便且可操作的方案以一锅三步级联方法合成寡肽的方法，该方法在溶液相肽合成中取得了进展，该方法通过化学选择性引入两个肽键。通过高效液相色谱法测定，三肽至六肽的总体收率很高（80-95％），几乎没有差向异构。本文所述的方法代表了一种更快，更容易和更温和的肽合成方法，并且以等摩尔量操作。该方案包括仲酰胺和叔酰胺的形成，并且与Z，Boc和Fmoc N保护基团以及D / L的使用兼容 和非蛋白氨基酸。