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

作者：Rodriguez Hortensia^*; Suarez Margarita; Albericio Fernando

来源：Journal of Peptide Science, 2010, 16(3): 136-140.

DOI：10.1002/psc.1209

• solid-phase peptide synthesis
• microwave
• Fmoc-N-methyl amino acids

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.

• 出版日期2010-3