作者:Regula von Eggelkraut-Gottanka、Annerose Klose、Annette G. Beck-Sickinger、Michael Beyermann
DOI:10.1016/s0040-4039(03)00582-3
日期:2003.4
simple Fmoc-based preparation of peptide αthioesters is presented. After Fmoc/t-butyl solid-phase synthesis on 2-chlorotrityl resin the C-terminal carboxylic group of the protected peptide is directly converted to the corresponding thioester. The method leads to very high yields, shows a low level of epimerization and can be easily applied also for the preparation of long peptide αthioesters as demonstrated
提出了一种高效且简单的基于Fmoc的肽α硫酯的制备方法。在2-氯三苯甲基树脂上进行Fmoc /叔丁基固相合成后,被保护肽的C-末端羧基直接转化为相应的硫酯。该方法的收率非常高,差向异构化程度很低,并且可以很容易地用于制备长肽α硫酯,如前神经肽Y的41个氨基酸N端片段(proNPY 1–40)所证明的那样。