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Backbone modified oligonucleotide analogs and preparation thereof through radical coupling

  • US 5,969,118 A
  • Filed: 02/04/1997
  • Issued: 10/19/1999
  • Est. Priority Date: 07/27/1990
  • Status: Expired due to Fees
First Claim
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1. A compound having structure:

  • ##STR8## wherein;

    Z1 is CH2 --RB, RB, CH2 --RA N═

    CH2, or RA N═

    CH2, provided that Z1 is not RA N═

    CH2 when X1 is H or OH, and Z1 is not RB when RB is OC(O)O--C6 H5 ;

    RA is O or NH;

    RB is a radical generating group selected from I, OC(O)O--C6 H5, OC(O)S--C6 H5, Se--C6 H5, O--C(S)O--C6 F5, O--C(S)O--C6 Cl5, O--C(S)O--(2,4,6--C6 Cl3), NO2, C(S)S--Me, C(S)O--(p--CH4 F), bis-dimethylglyoximato-pyridine cobalt, O--C(S)C6 H5, O--C(S)SCH3, O--C(S)-imidazole, and C(O)O-pyridin-2-thione;

    Y1 is H, hydroxymethyl, a nucleoside, a nucleotide, an oligonucleotide, an oligonucleoside, or a hydroxyl-protected or amine-protected derivative thereof;

    BX1 is a nucleosidic base;

    Q1 is O, S, CH2, CHF or CF2 ; and

    X1 is H, OH, C1 to C10 lower alkyl, substituted lower alkyl, alkaryl or aralkyl, F, Cl, Br, CN, CF3, OCF3, OCN, O-alkyl, S-alkyl, N-alkyl, O-alkenyl, S-alkenyl, N-alkenyl, SOCH3, SO2 CH3, ONO2, NO2, N3, NH2, heterocycloalkyl, heterocycloalkaryl, aminoalkylamino, polyalkylamino or substituted silyl.

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