Diels-Alder cycloadditions in water for the straightforward preparation of peptide–oligonucleotide conjugates |
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Authors: | Vicente March n, Samuel Ortega, Daniel Pulido, Enrique Pedroso, Anna Grandas |
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Affiliation: | Vicente Marchán, Samuel Ortega, Daniel Pulido, Enrique Pedroso, and Anna Grandas |
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Abstract: | The Diels-Alder reaction between diene-modified oligonucleotides and maleimide-derivatized peptides afforded peptide–oligonucleotide conjugates with high purity and yield. Synthesis of the reagents was easily accomplished by on-column derivatization of the corresponding peptides and oligonucleotides. The cycloaddition reaction was carried out in mild conditions, in aqueous solution at 37°C. The speed of the reaction was found to vary depending on the size of the reagents, but it can be completed in 8–10 h by reacting the diene-oligonucleotide with a small excess of maleimide-peptide. |
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