Abstract
N-Methylation may positively influence the pharmacokinetic properties of peptides by improving oral availability and in vivo half-life. Additionally, target affinity and specificity may be improved. Here, we describe the solid-phase N-methylation of peptides using direct alkylation. This method allows a rapid N-methyl scan of synthetic, bioactive peptides. Additionally, a microwave-enhanced method for the difficult coupling onto the methylated N terminus is provided.
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Roodbeen, R., Jensen, K.J. (2013). Synthesis of N-Methylated Peptides: On-Resin Methylation and Microwave-Assisted Couplings. In: Jensen, K., Tofteng Shelton, P., Pedersen, S. (eds) Peptide Synthesis and Applications. Methods in Molecular Biology, vol 1047. Humana Press, Totowa, NJ. https://doi.org/10.1007/978-1-62703-544-6_10
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DOI: https://doi.org/10.1007/978-1-62703-544-6_10
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