Abstract
Novartis Pharmaceuticals, Central Research Laboratories, Hulley Road, Macclesfield, Cheshire, SK10 2NX, UKFax +44(1403)323307; E-mail: robin.fairhurst@pharma.novartis.comReceived 29 January 2002Synlett 2002, No. 5, 03 05 2002. Article Identifier: 1437-2096,E;2002,0,05,0763,0766,ftx,en;D01702ST.pdf. © Georg Thieme Verlag Stuttgart · New YorkISSN 0936-5214Abstract: The preparation of thymidine-thymidine and thymidine-5-methylcytidine dinucleosides containing a 3 -C-P-N-5 ethylphosphonamidate ester linkage, with defined phosphorus stere-ochemistry, in combination with a 2 -methoxy substituent in thelower sugar residue, is described. Incorporation of these dinucleo-sides into DNA oligonucleotides and the effect upon duplex stabil-ity with complimentary RNA is reported.Key words: antisense, modified oligonucleotides, nucleosides,phosphorus, stereoselective
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