Modified oligonucleotides and intermediates useful in nucleic ac

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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C07H 2104

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056250509

ABSTRACT:
The present invention provides nuclease resistant 3'-carbon modified oligonucleotides that can be used in the field of nucleic acid therapeutics and diagnostics. The modified oligonucleotides of the present invention have at least one modified internucleotide linkage wherein the divalent oxygen moiety at the 3'-position of the internucleotide linkage is replaced by a tetravalent carbon moiety. The 3'-carbon modified internucleotide linkage is preferably a 3'-methylene or 3'-hydroxymethylene linkage. Also provided are a method and monomeric nucleoside and nucleotide intermediates for making the modified oligonucleotides of the present invention.

REFERENCES:
Heinemann et al., Nucleic Acids Research (1991), vol. 19 (3): pp. 427-433.
Mazur et al., Tetrahedron (1984), vol. 40 (20): pp. 3949-3956.
Crockett, Aldrichimica (1983), vol. 16 (3): pp. 47-56.
Morr et al., GBF Monogr. Ser., 8(Chem. Synth. Mol. Biol.) 1987, pp. 107-113.
Bjergarde et al., Nucleic Acids Research 19, 1991, 5843-5850.
Worms et al, in. Organic Phosphorus Compounds, vol 7, Edited Kosolapoff and Maier, p. 30, 1976.

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