Abstract

LNA (Locked Nucleic Acids) is a novel oligonucleotide analogue containing [2.2.1]bicyclo nucleoside monomers. A novel and significantly improved method for convergent synthesis of LNA [2.2.1]bicyclo nucleosides using a 4-C-tosyloxymethyl-1, 2-di-O-acetyl furanose as a key synthon is described. In addition, an alternative, robust linear approach allowing selective formation of the desired [2.2.1]bicyclo LNA nucleosides via a tricyclic nucleoside intermediate is introduced.

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