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Novel conformationally locked nucleosides and nucleotides
 Nencka, Radim ; Šála, Michal ; Hřebabecký, Hubert ; Procházková, Eliška ; Mackman, R. ; Barauskas, O. ; Lee, Y. J. ; Tian, Y.
We report on a synthesis of two novel types of conformationally locked nucleoside analogues. We prepared 7 membered ring 3’,5’-bridged nucleoside analogs locked in a Southern conformation. These nucleoside analogues were converted in one pot to appropriate phosphoramidate prodrugs using boronate methodology. We also devised and prepared a novel carbocyclic nucleoside by replacing furanose with cyclohexene that resulted in a locked Northern conformation similar to LNA monomers. Further details on the biological activity and application for oligonucleotide synthesis will be discussed in detail.
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