Process for the preparation of phosphorothioate...

Details Process for the preparation of phosphorothioate... Process for the preparation of phosphorothioate...

C - Chemistry, Metallurgy

07

H

C07H 21/00 (2006.01) C07H 21/04 (2006.01)

Patent

CA 2437040

A process for the synthesis of phosphorothioate oligonucleotides is provided which comprises assembling an aligonucleotide bound to to a solid support in the presence of acetonitrile; prior to cleaving the oligonucleotide from the solid support removing the acetonitrile; and cleaving the oligonucleotide from the solid support. The process is particularly suited to the large scale synthesis of nucleotides. The acetonitrile may be removed from the solid support by one or both to drying and by washing with solvents. Preferred washing solvents comprise trialkylamines.

L'invention concerne un procédé de synthèse d'oligonucléotides phosphorothioate qui consiste à assembler un complexe aligonucléotide à un support solide en présence d'acétonitrile, avant le clivage de l'oligonucléotide du support solide en retirant l'acétonitrile et en clivant l'oligonucléotide du support solide. Ce procédé est adapté en particulier à la synthèse à grande échelle de nucléotides. On peut retirer l'acétonitrile du support solide par séchage et/ou lavage au moyen de solvants. Les solvants de lavage utilisés de préférence contiendront des trialkylamines.

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