Process for the preparation of nucleosides

Organic compounds -- part of the class 532-570 series – Organic compounds – Carbohydrates or derivatives

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536 2531, 536 2533, 536 2621, 536 2671, 536 284, 536 2854, 536 286, C07H 2100, C07H 2102, C07H 1904, C07H 19056

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active

052684644

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 R.sub.1 --O--, wherein R.sub.1 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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patent: 5134228 (1992-07-01), Takaku

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