Pyrimidine nucleoside compounds and oligonucleoside compounds co

Details Pyrimidine nucleoside compounds and oligonucleoside compounds co Pyrimidine nucleoside compounds and oligonucleoside compounds co

1994-03-11

2000-05-09

Wilson, James O.

Organic compounds -- part of the class 532-570 series

Organic compounds

Carbohydrates or derivatives

536 221, 536 253, 536 2532, 536 268, 536 281, 536 284, 536 285, 536 2851, 536 2852, 536 2853, 536 2854, 536 2855, C07H 1906, C07H 2100

Patent

active

060605928

ABSTRACT:
Novel 2- and 4-substituted pyrimidine nucleosides and oligonucleosides are provided, as are methods and intermediates useful in preparing same. In preferred embodiments, one of the 2- and 4-substituents is .dbd.O, .dbd.NH, or .dbd.NH.sub.2.sup.+ and the other is Q, .dbd.C (R.sub.A)--Q, C(R.sub.A)(R.sub.B)--C(R.sub.C)(R.sub.D)--Q, C (R.sub.A).dbd.C(R.sub.C)--Q or C.tbd.C--Q, where R.sub.A, R.sub.B, R.sub.C and R.sub.D independently are H, SH, OH, NH.sub.2, or C.sub.1 -C.sub.20 alkyl, or one of (R.sub.A)(R.sub.B) or (R.sub.C)(R.sub.D) is .dbd.O, and Q is halogen, hydrogen, C.sub.1 -C.sub.20 alkyl, C.sub.1 -C.sub.20 alkylamine, C.sub.1 -C.sub.20 alkyl-N-phthalimide, C.sub.1 -C.sub.20 alkylimidazole, C.sub.1 -C.sub.20 alkylbis-imidazole, imidazole, bis-imidazole, amine, N-phthalimide, C.sub.2 -C.sub.20 alkenyl, C.sub.2 -C.sub.20 alkynyl, hydroxyl, thiol, keto, carboxyl, nitrates, nitro, nitroso, nitrile, trifluoromethyl, trifluoromethoxy, O-alkyl, S-alkyl, NH-alkyl, N-dialkyl, O-aralkyl, S-aralkyl, NH-aralkyl, azido, hydrazino, hydroxylamino, isocyanato, sulfoxide, sulfone, sulfide, disulfide, silyl, O-(hydroxyl protecting group), a leaving group, a heterocycle, an intercalator, a reporter molecule, a conjugate, a polyamine, a polyamide, a polyethylene glycol, a polyether, or a depurination enhancing group.

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