
Automated Synthesis of Head-to-Tail Cyclic Peptides via Microwave-Enhanced SPPS
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Summary
Fully automated synthesis of head-to-tail cyclized peptides can be performed rapidly and with excellent purity using the Liberty Blue and Liberty PRIME peptide synthesizers. Microwave SPPS benefits not only the linear assembly but also the subsequent cyclization step with exceptional purity achieved on a variety of difficult biologically important peptides. The one-pot Fmoc SPPS cycles used on the Liberty PRIME provide even further benefit for synthesis time and waste reduction.
Table 1: Fully automated synthesis of head-to-tail cyclized peptides.
Instrument | Sequence | Crude Purity | Synthesis Time |
Liberty Blue | cyclo-[GVYLHIE] | 78% | 2 h 13 min |
Liberty Blue | cyclo-[WTaRRR-nal-R-Fpa-nle-Q] | 75% | 3 h 1 min |
Liberty PRIME | cyclo-[WTaRRR-nal-R-Fpa-nle-Q] | 75% | 2 h |
Liberty PRIME |
cyclo-[WTaR-NMeGly-NMePhe-nal-NMeGly-Fpa-nle-E] |
66% | 2 h 5 min |
Liberty PRIME |
cyclo-[KA-NMeIle-NMeGly-NMeLeu-ANMeGly-NMeGly-E] |
73% | 2 h 12 min |
Table 2: Comparison of Liberty Blue and Liberty PRIME for the Synthesis of Cyclorasin A
Instrument | Peptide | Synthesis Time | Total Waste Volume |
Liberty Blue | Cyclorasin A | 3 h 1 min | 674 mL |
Liberty PRIME | Cyclorasin A | 2 h | 584 mL |