Oligonucleotide conjugates by means of copper-free click chemistry - Expanding the repertoire of strained cyclooctyne phosphoramidites

Article abstract of DOI:10.1055/s-0030-1260104

A set of four phosphoramidite building blocks containing a strained dibenzocyclooctyne moiety is reported, including one example equipped with a cleavable disulfide linker. Application of these amidites in solid-phase oligonucleotide synthesis yields either 5′- or 3′-cyclooctyne- modified nucleic acids. The strained cyclooctyne-bearing oligonucleotides are used in rapid and clean conjugation reactions with azide-containing (bio)molecules. Georg Thieme Verlag Stuttgart - New York.