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 2714353

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

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