A convenient microwave‐enhanced solid‐phase synthesis of short chain N‐methyl‐rich peptides |
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| Authors: | Hortensia Rodríguez Margarita Suarez Fernando Albericio |
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| Institution: | 1. Institute for Research in Biomedicine, Barcelona Science Park, Baldiri Reixac 10, 08028‐Barcelona, Spain;2. Laboratorio de Síntesis Orgánica, Facultad de Quimica, Universidad de La Habana, 10400‐Ciudad Habana, Cuba;3. CIBER‐BBN, Networking Centre on Bioengineering, Biomaterials and Nanomedicine, Barcelona Science Park, Baldiri Reixac 10, 08028‐Barcelona, Spain;4. Department of Organic Chemistry, University of Barcelona, MartíiFranqué 1‐10, 08028‐Barcelona, Spain |
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| 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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| Keywords: | solid‐phase peptide synthesis microwave Fmoc‐N‐methyl amino acids |
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