Synthesis by Microwave-assisted Orthogonal
Microwave heating is conducive to the synthesis of peptide nucleic acids and provides a fully automated and efficient synthesis strategy for PNA-peptide conjugates. Creative Peptides has been producing high quality custom PNAs, including PNA-peptide conjugates. Through the strategy of microwave heating orthogonal to chemical methods, we provide our customers with high purity, high quality synthetic products that meet each customer's expectations in a time frame.
Solid-phase synthetic chemical methods are generally time-consuming and non-automated, so have certain limitations on the wider application of PNA in chemistry and biology. However, as a non-traditional energy method, microwave can increase the reaction rate by hundreds or even thousands of times, and has the advantages of convenient operation, few by-products, high yield and easy separation and purification, and it tends to meet the environmental friendliness of "green synthesis" needs. Microwave heating facilitates peptide nucleic acid synthesis offering a fully automated and efficient synthetic strategy to PNA–peptide conjugates.
Fig. 1 Synthesis of PNA–peptide conjugates by microwave-assisted orthogonal (Svensen N. et al.2008)
PNA–peptide synthesis was carried out in an automated CEM peptide synthesizer.
- Dde-deprotection was carried out under either acidic (20% NH2OH·HCl/imidazole 1:0.75 in NMP/DMF 5:1) or more traditional basic conditions (20% NH2OH·H2O/imidazole 1:0.75 in NMP/DMF 5:1) under microwave irradiation.
- PNA monomer coupling was mediated using pre-activated monomers (0.22 M Dde-monomer, 5.5 equiv) in DMF, mixed with 0.20 M PyBOP (5 equiv) also in DMF and with NEM (11 equiv) for 1 min and microwave irradiation for 20 min at 60 oC.
- The PNA–peptide conjugate was synthesized using the slightly acidic conditions for Dde removal (20% NH2OH·HCl/imidazole 1:0.75 in NMP/DMF 5:1), and Fmoc-deprotection and amino acid couplings were carried out according to standard literature procedures.
- Following Fmoc-synthesis, the peptide was capped with acetic anhydride/pyridine (1:1) for 20 min, before the PNA was capped with 5(6)-carboxyfluorescein.
- The peptide–PNA conjugates were cleaved from the solid support with TIS/TFA19 and purified by RP-HPLC.
- High-quality synthetic products and complete product analysis reports
- Shortest delivery cycle
- High-purity, customizable products
Creative Peptides is committed to the development and synthesis of PNA conjugates. With our advanced operating facilities and experienced research team, we are confident that we can complete your PNA studies and provide accurate and timely results. If you would like to know more, please feel free to contact us.
- Svensen N. et al.Microwave-assisted orthogonal synthesis of PNA-peptide conjugates. Tetrahedron Letters, 2008, 49(46):6498-6500.
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