用于肽合成的肟铯盐裂解剂的制备及性能

Preparation of Oxime Cesium Salts and Its Function as Cleaving Agents in Peptide Synthesis

以获得侧链全保护的多肽为总目标,选择接入溴乙酰基把手的Wang树脂作为固相载体,采用多肽固相合成法制备了3种模型肽,将其用于对具有弱碱性和强亲核性的肟盐类裂解剂的研究;设计并制备了5种不同结构的肟铯盐,将其用于模型肽的裂解,并选择综合效果最好的2-吡啶甲醛肟铯盐进行裂解条件的优化.结果表明,肟铯盐类裂解剂可以温和、高效地裂解模型肽,得到侧链全保护的多肽.

This paper aimed at preparation of side chain protected peptides. Modified Wang resin loaded with2-bromoacetyl linker was selected for syntheses of three kinds of model peptides by the method of solid phase peptide synthesis（ SPPS）. These model peptides were used to examine the cleave function of some oximates with alkalescence and strong nucleophilicity. Five oxime cesium salts with different structures were designed and synthesized for the cleavage of model peptides from the resin. The optimal cleave conditions of 2-pyridine aldoxime cesium which had the best performance in the cleavage,was studied in detail. The experimental results showed that model peptides with side chain fully protected could be obtained with high yields in mild conditions using oxime cesium salts as cleave reagents in SPPS.