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A convenient microwave-enhanced solid-phase synthesis of short chain N-methyl-rich peptides

✍ Scribed by Hortensia Rodríguez; Margarita Suarez; Fernando Albericio

Publisher
John Wiley and Sons
Year
2010
Tongue
English
Weight
633 KB
Volume
16
Category
Article
ISSN
1075-2617

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✦ Synopsis

Abstract

Structural modification of the peptide backbone via N‐methylation is a powerful tool to modulate the pharmacokinetic profile and biological activity of peptides. Here we describe a rapid and highly efficient microwave(MW)‐assisted Fmoc/tBu solid‐phase method to prepare short chain N‐methyl‐rich peptides, using Rink amide p‐methylbenzhydrylamine (MBHA) resin as solid‐phase support. This method produces peptides in high yield and purity, and reduces the time required for Fmoc‐N‐methyl amino acid coupling. Copyright © 2010 European Peptide Society and John Wiley & Sons, Ltd.

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