Robust Chemical Synthesis of "Difficult Peptides" via 2-Hydroxyphenol-pseudoproline (ψ2-hydroxyphenolpro) Modifications.
J Org Chem
; 89(5): 3143-3149, 2024 03 01.
Article
em En
| MEDLINE
| ID: mdl-38373048
ABSTRACT
The challenging preparation of "difficult peptides" has always hindered the development of peptide-active pharmaceutical ingredients. Pseudoproline (ψpro) building blocks have been proven effective and powerful tools for the synthesis of "difficult peptides". In this paper, we efficiently prepared a set of novel 2-(oxazolidin-2-yl)phenol compounds as proline surrogates (2-hydroxyphenol-pseudoprolines, ψ2-hydroxyphenolpro) and applied it in the synthesis of many well-known "difficult peptides", including human thymosin α1, amylin, and ß-amyloid (1-42) (Aß42).
Texto completo:
1
Base de dados:
MEDLINE
Assunto principal:
Tiazóis
/
Prolina
/
Catecóis
Limite:
Humans
Idioma:
En
Ano de publicação:
2024
Tipo de documento:
Article