Abstract
With the current interest in anti-sense and anti-gene technologies, an efficient, fast and less toxic synthesis protocol would be advantageous for the oligomerisation of Peptide Nucleic Acids (PNA). Most of the methods currently in use for the t-Boc synthesis of PNA's use TFA/m-cresol, pyridine, piperidine and capping reagents. In this work, a rapid synthesis protocol has been adapted from an earlier published peptide synthesis method allowing a reduction in cycle time from around 30 min down to 16 min. By utilising quantitative deprotection with 100% TFA, a coupling time of 10 min and a four-fold excess of monomer, this synthesis protocol has been used to synthesise a number of PNA's incorporating all four nucleotides of varying sequence, up to 17 residues in length.
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Vearing, C.J., Fecondo, J.V. A rapid coupling protocol for the synthesis of peptide nucleic acids. Letters in Peptide Science 9, 211–219 (2002). https://doi.org/10.1023/A:1024187414586
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DOI: https://doi.org/10.1023/A:1024187414586