Efficient Synthesis of DNA Conjugates by Strain‐Promoted Azide–Cyclooctyne Cycloaddition in the Solid Phase

Abstract

AbstractConjugation of ligands to DNA oligonucleotides has been achieved in the solid phase by strain‐promoted azide–alkyne cycloaddition (SPAAC). The oligonucleotide, modified with a simple nonfluroinated, monocyclic octyne, efficiently forms conjugates with a range of azide dipoles with varying steric and electronic characteristics. The reaction is clean and easily executed in a copper free environment at room temperature. It provides a variety of triazole‐linked nucleic acid conjugates and is potentially useful in biotechnology and cell biology.