Process for the preparation of nucleosides
First Claim
1. A process for the preparation of natural or synthetic nucleosides, nucleoside analogs or oligonucleotides from at least two such nucleosides and/or nucleoside analogs whose basic molecule contains an unsubstituted or substituted radical of a nucleic base B and a protected hydroxyl group of formula R1 --O--, wherein R1 is a protective group, or which are linked to the oxygen atom of a hydroxyl group direct or to a solid support through a linking group, from nucleoside monomers or from oligonucleotides to the basic molecule of which, in addition to said radicals, a group of formula I, Ia or Ib ##STR6## is attached, by converting the group of formula I, Ia or Ib into a hydroxyl group --OH by reacting the nucleosides or oligonucleotides, in the absence or presence of an inert organic solvent, with an excess of an aliphatic, cycloaliphatic araliphatic or aromatic alcohol containing 1 to 30 carbon atoms, a polyol containing 2 to 50 carbon atoms or a polymeric polyol, in the presence of at least a catalytic amount of an inorganic base or of an organic nitrogen base, which base has a pK value of 4 to 10.
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Abstract
A process for the preparation of natural or synthetic nucleosides, nucleoside analogs or oligonucleotides from at least two such nucleosides and/or nucleoside analogs whose basic molecule contains an unsubstituted or substituted radical of a nucleic base B and a protected hydroxyl group of formula R1 --O--, wherein R1 is a protective group, or which are linked to the oxygen atom of a hydroxyl group direct or to a solid support through a linking group, from nucleoside monomers or from oligonucleotides to the basic molecule of which, in addition to said radicals, a group of formula I, Ia or Ib ##STR1## is attached, by converting the group of formula I, Ia or Ib into a hydroxyl group --OH by reacting the nucleosides or oligonucleotides, in the absence or presence of an inert organic solvent, with an excess of an aliphatic, cycloaliphatic araliphatic or aromatic alcohol containing 1 to 30 carbon atoms, a polyol containing 2 to 50 carbon atoms or a polymeric polyol, in the presence of at least a catalytic amount of an inorganic base or of an organic nitrogen base, which base has a pK value of 4 to 10.
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Citations
36 Claims
- 1. A process for the preparation of natural or synthetic nucleosides, nucleoside analogs or oligonucleotides from at least two such nucleosides and/or nucleoside analogs whose basic molecule contains an unsubstituted or substituted radical of a nucleic base B and a protected hydroxyl group of formula R1 --O--, wherein R1 is a protective group, or which are linked to the oxygen atom of a hydroxyl group direct or to a solid support through a linking group, from nucleoside monomers or from oligonucleotides to the basic molecule of which, in addition to said radicals, a group of formula I, Ia or Ib ##STR6## is attached, by converting the group of formula I, Ia or Ib into a hydroxyl group --OH by reacting the nucleosides or oligonucleotides, in the absence or presence of an inert organic solvent, with an excess of an aliphatic, cycloaliphatic araliphatic or aromatic alcohol containing 1 to 30 carbon atoms, a polyol containing 2 to 50 carbon atoms or a polymeric polyol, in the presence of at least a catalytic amount of an inorganic base or of an organic nitrogen base, which base has a pK value of 4 to 10.
Specification