Patent ID: 9701708
Date: 2017-07-11
CPC Classifications: C07H

Claim:
1. A method of coupling solid support bound free hydroxyl groups to bicyclic nucleosides of Formula I: wherein for each bicyclic nucleoside of Formula I: Bx is an optionally protected heterocyclic base moiety; T T one of Q comprising treatment of the free hydroxyl groups with a coupling reagent which is about 70% by volume activator solution consisting of 1.0 molar 4,5-dicyanoimidazole and about 0.1 molar N-methylimidazole in acetonitrile and about 30% by volume of a solution having about a 0.2 molar concentration of bicyclic nucleosides of Formula I disolved in acetonitrile or a mixture of acetonitrile and toluene and wherein the volume of coupling reagent added provides about 1.75 equivalents of bicyclic nucleosides of Formula I based on the initial loading of the solid support with free hydroxyl groups.