A PROCESS FOR THE SYNTHESIS OF MODIFIED P-CHIRAL NUCLEOTIDE ANALOGUES

摘要

The diastereomer form that the modification P-chiral nucleotide analogs general formula (1) of technique synthesis is pure possesses predetermined configuration P-atom; in attached drawing: R1 represents blocking group; it is preferred that 4,4 '-dimethoxytrityl (DMT), 9-phenylxanthene-9-ol (under) or trialkylsilkl group; R2 is the hydroxyl of hydrogen atom, protection; halogen, chlorine alkyl; nitrile; azide; protect amido; perfluoroalkyl (contains at most 4 carbon atoms); perfluoroalkoxyl (contains at most 4 carbon atoms and up to nine fluorine or chlorine atom); alkoxyalkyl; vinyl, acetenyl, OQ1, SQ1, NHQ1; wherein Q1 is represented alkyl (C1-C4), aryl (C6-C12), alkenyl (C3-C12) or alkynyl (C3-C12); B represents purine or pyrimidine bases and suitably protects at nitrogen-atoms (if necessary); Z is selected from Q1 or vinyl, acetenyl, amino methyl or aminoethyl substituent group; X indicates oxygen atom, sulphur atom or selenium atom; Rx blocking groups, preferably aroyl, acyl group, alkoxy carbonyl, benzene sulfonic acid, the elongated oligonucleotide chain of alkyl, trialkylsilkl group or next unit. Antisense oligonucleotides, the compound (1) of the general formula containing P-chiral have the hybridization of enhancing and transmit property.