Process for the preparation of oligonucleotides

Details Process for the preparation of oligonucleotides Process for the preparation of oligonucleotides

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) B01J 19/00 (2006.01)

Patent

CA 2510477

A process for the synthesis of an oligonucleotide is provided in which an oligonucleotide is assembled on a swellable solid support using the phosphoramidite approach in the presence of an activator, wherein the activator is not tetrazole or a substituted tetrazole. Preferred activators are pyridinium, imidazolinium and benzimidazolinium salts; benzotriazole and derivatives thereof; and saccharin or a saccharin derivative. Preferred swellable solid supports comprise functionalised polystyrene, partially hydrolysed polyvinylacetate or poly(acrylamide).

L'invention concerne un procédé de synthèse d'un oligonucléotide. Selon ce procédé, un oligonucléotide est assemblé sur un support solide dilatable par la méthode à la phosphoramidite, en présence d'un activateur autre que tétrazole et tétrazole substitué. Des activateurs préférés sont pyridinium, imidazolinium et des sels de benzimidazolinium; benzotriazole et ses dérivés; et saccharine ou un dérivé de saccharine. Des supports solides dilatables préférés comprennent polystyrène fonctionnalisé, polyvinylacetate partiellement hydrolysé ou poly(acrylamide).

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