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filingDate 1998-04-23-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_da0ae1760d071e605a0a13ab50bf478d
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publicationDate 1998-11-05-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber WO-9849179-A2
titleOfInvention A process for the synthesis of modified p-chiral nucleotide analogues
abstract The process for the synthesis of modified P-chiral nucleotide analogues of general formula (1) in the form of pure diastereomer possessing preselected configuration at the P-atom, where: R1 stands for a protecting group, preferably 4,4'-dimethoxytrityl (DMT), 9-phenylxanthene-9-ol (Px) or trialkylsilyl group; R2 is a hydrogen atom, protected hydroxyl group, halogen, chloroalkyl, nitrile, azide, protected amine group, perfluoroalkyl (containing up to four carbon atoms), perfluoroalkoxyl (containing up to four carbon atoms and up to nine fluorine or chlorine atoms), alkoxyalkyl, vinyl, ethynyl, OQ1, SQ1, NHQ1, where Q1 stands for alkyl (C1-C4), aryl (C6-C12), alkenyl (C3-C12) or alkynyl (C3-C12); B stands for a purine or pyrimidine base (appropriately protected at nitrogen atoms if necessary); Z is selected from Q1 or vinyl, ethynyl, aminomethyl or aminoethyl substituents; X means an oxygen, sulfur or selenium atom; Rx is a protecting group, preferably aroyl, acyl, alkoxycarbonyl, benzenesulfonic, alkyl, trialkylsilyl group or the next unit of elongated oligonucleotide chain. Antisense oligonucleotides containing P-chiral compounds of general formula (1) have enhanced hybridization and transporting properties.
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priorityDate 1997-04-25-04:00^^<http://www.w3.org/2001/XMLSchema#date>
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