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A convenient microwave‐enhanced solid‐phase synthesis of short chain N ‐methyl‐rich peptides
Author(s) -
Rodríguez Hortensia,
Suarez Margarita,
Albericio Fernando
Publication year - 2010
Publication title -
journal of peptide science
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.475
H-Index - 66
eISSN - 1099-1387
pISSN - 1075-2617
DOI - 10.1002/psc.1209
Subject(s) - solid phase synthesis , phase (matter) , chemistry , microwave , chain (unit) , combinatorial chemistry , peptide , biochemistry , organic chemistry , physics , quantum mechanics , astronomy
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.