Abstract
A novel approach to the synthesis of peptide-oligonucleotide conjugates (POC) based on the oxathiaphospholane chemistry has been developed. Peptide and oligonucleotide fragments, which were separately prepared, were linked postsynthetically by the functionalization of the peptide either by attachment of the oxathiaphospholane residue directly at the N-terminus or at the hydroxy group of the linker connected to N-terminus. The conjugation reaction, based on DBU-assisted nucleophilic attack of hydroxy group of oligonucleotide on phosphorus atom in the oxathiaphospholane derivatives of peptide, furnished the desired POC.
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