Peptide αthioester formation using standard Fmoc-chemistry

Autor: Annette G. Beck-Sickinger, Regula von Eggelkraut-Gottanka, Annerose Klose, Michael Beyermann
Rok vydání: 2003
Předmět:
Zdroj: Tetrahedron Letters. 44:3551-3554
ISSN: 0040-4039
DOI: 10.1016/s0040-4039(03)00582-3
Popis: A highly efficient and 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 for the 41 amino acid N-terminal fragment of pro-neuropeptide Y (proNPY 1–40).
Databáze: OpenAIRE