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Christensen, L; Fitzpatrick, R; Gildea, B; Petersen, K H; Hansen, H F; Koch, T; Egholm, M; Buchardt, O; Nielsen, P E; Coull, J; Berg, R H
Journal of peptide science, May/June 1995, Letnik: 1, Številka: 3Journal Article
Peptide nucleic acids (PNA) were synthesized by a modified Merrifield method using several improvements. Activation by O-benzotriazol-1-yl-1,1,3,3-tetramethyluronium hexafluorophosphate in combination with in situ neutralization of the resin allowed efficient coupling of all four Boc-protected PNA monomers within 30 min. HPLC analysis of the crude product obtained from a fully automated synthesis of the model PNA oligomer H-CGGACTAAGTCCATTGC-Gly-NH2, indicated an average yield per synthetic cycle of 97.1%. N1-benzyloxycarbonyl-N6(3)-methylimidazole triflate substantially outperformed acetic anhydride as a capping reagent. The resin-bound PNAs were successfully cleaved by the 'low-high' trifluoromethanesulphonic acid procedure.
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