Method for the synthesis of oligonucleotide derivatives

C - Chemistry – Metallurgy – 07 – H

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C07H 21/00 (2006.01) A61K 31/7088 (2006.01)

Patent

CA 2650668

Method for the synthesis of nucleotide derivatives wherein molecules of interest are grafted on the oligonucleotide with the help of a "click chemistry" reaction between an azide function on the molecule of interest and an alkyne function on the oligonucleotide, or between an alkyne function on the molecule of interest and an azide function on the oligonucleotide. Intermediate molecules, notably alkyne functionalized oligonucleotides, grafted oligonucleotides, azide functionalized oligonucleotides, oligonucleotide micro arrays containing them and the use of those grafted oligonucleotides for biological investigation and for cell targeting.

L'invention concerne un procédé de synthèse de dérivés nucléotidiques dans lequel des molécules d'intérêt sont greffées sur l'oligonucléotide à l'aide d'une réaction de "click chemistry" entre une fonction azide sur la molécule d'intérêt et une fonction alcyne sur l'oligonucléotide, ou entre une fonction alcyne sur la molécule d'intérêt et une fonction azide sur l'oligonucléotide. L'invention concerne également des molécules intermédiaires, notamment des oligonucléotides fonctionnalisés par un alcyne, des oligonucléotides greffés, des oligonucléotides fonctionnalisés par un azide, des microréseaux oligonucléotidiques les contenant, ainsi que l'utilisation de ces oligonucléotides greffés pour l'étude biologique et pour le ciblage cellulaire.

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