Laboratorio Química Farmacéutica, Departamento de Química Orgánica, Facultad de Química, Universidad de la República, Montevideo, Uruguay.
Methods Mol Biol. 2022;2371:3-17. doi: 10.1007/978-1-0716-1689-5_1.
Lactamization is the key step in the synthesis of many compounds with macrocyclic structure. As the interest for these types of molecules grows in various fields such as drug discovery and nanomaterials, different methodologies to access them are being developed. Three different strategies to obtain cyclic peptides via lactamization are described in this chapter: solution-phase macrocyclization following solid-phase peptide synthesis (SPPS) of the linear precursor, SPPS and on-resin cyclization on the 2-chlorotrityl chloride (2-CTC) resin, and SPPS and on-resin cyclization by native chemical ligation on the amino-PEGA resin.
成环反应是许多具有大环结构的化合物合成的关键步骤。随着人们对这些类型的分子在药物发现和纳米材料等各个领域的兴趣不断增长，正在开发不同的方法来获得它们。本章描述了通过成环反应获得环肽的三种不同策略：固相肽合成（SPPS）线性前体后在溶液相中进行大环化、2-氯三苯甲基氯（2-CTC）树脂上的 SPPS 和树脂内环化、以及氨基-聚乙二醇（PEGA）树脂上的 SPPS 和树脂内通过天然化学连接进行环化。
