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Activators for oligonucleotide synthesis

  • US 6,846,922 B1
  • Filed: 11/08/2000
  • Issued: 01/25/2005
  • Est. Priority Date: 06/02/1998
  • Status: Expired due to Fees
First Claim
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1. A method for the preparation of a compound of formula:

  • embedded imagewherein;

    R1 is a nucleoside or an oligonucleotide;

    R2 is a nucleoside linked to a solid support, or an oligonucleotide linked to a solid support;

    Pg is a phosphorus protecting group;

    comprising;

    providing a phosphoramidite of formula;

    embedded image

    wherein R6 is —

    N(R7)2 wherein R7 is alkyl having from one to about six carbons;

    or R7 is a heterocycloalkyl or heterocycloalkenyl ring containing from 4 to 7 atoms, and having up to 3 heteroatoms selected from nitrogen, sulfur, and oxygen; and

    reacting said phosphoramidite with a hydroxyl group of a nucleoside linked to a solid support, or an oligonucleotide linked to a solid support;

    said reaction being performed in the presence of an activating reagent, said activating reagent comprising at least one pyridinium salt and at least one substituted imidazole.

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