Method for preparing oligonucleotides

Ilaria Adamo , Cécile Dueymes , Andreas Schönberger (1) , Jean-Louis Imbach , Albert Meyer (2) , François Morvan (2) , Jean-Jacques Vasseur (2) , Meinolf Lange (1) , Fritz Link (1)

1 GIRENDUS
2 IBMM - Institut des Biomolécules Max Mousseron [Pôle Chimie Balard]

A solution phase synthesis method for preparing an oligonucleotide, wherein at least some of the reagents are solid supported. The method suitable for large- scale synthesis comprises coupling a protected compound with a nucleotide derivative having a protection group in the presence of a solid supported activator to give an elongated oligonucleotide with a P(III)-internucleotide bond; optionally processing the elongated oligonucleotide by capping by reaction with a solid supported capping agent and/or by oxidizing or sulfurizing by reaction of the oligonucleotide with a solid supported oxidizing or sulfurization reagent, and removing the protection group. The coupling may include reacting and 3'-protected compound of formula: with a nucleotide derivative having a 5'-protection group, or reacting a 5'-protected compound of formula

Domaines: Chimie organique

Ilaria Adamo, Cécile Dueymes, Andreas Schönberger, Jean-Louis Imbach, Albert Meyer, et al.. Method for preparing oligonucleotides. France, Patent n° : US 20110224424A1. 2011. ⟨hal-00630206⟩