Verfahren zur Herstellung eines Oligonukleotids

Details

Veröffentlichungs-Nr.

EP4755898

Anmeldetag

2. August 2024

Veröffentlichung

6. Februar 2025

Rechtsraum

EP

IPC

C07H21/04

Abstract

The purpose of the present invention is to provide a method for producing an oligonucleotide, wherein the amount of nucleoside phosphoramidite remaining in a reaction vessel is suppressed and the amount of used nucleoside phosphoramidite is reduced. The abovementioned problem is solved by, inter alia, a method for producing an oligonucleotide, the method comprising: (a) a step for detaching a protective group from a protected nucleoside where the protective group is bonded to a hydroxyl group, a thiol group, or an amino group at the 3' position or the 5' position; (b) a step for, in the presence of an activator, bonding a nucleoside phosphoramidite to the hydroxyl group, thiol group, or amino group at the 3' position or the 5' position of the nucleoside from which the protective group has been detached; (c) a step for sulfurizing or oxidizing the bond formed by step (b); and (d) a step for capping the hydroxyl group, thiol group, or amino group at the unbonded 3' position or 5' position of the nucleoside, wherein the capping of step (d) includes the operation of causing the nucleoside and a capping solution to come into contact for only a prescribed period of time [T] (minutes), the capping solution includes N-methyl imidazole at a blending rate of [N] (%) (the room temperature volume percentage (%) of unblended N-methyl imidazole with respect to the unblended room temperature total volume (100%) of reagents blended as capping solution components), and the product ([N] ×[T]) of [N] and [T] is 0.5 to 3.0.

Anmelder

Firma

Nitto Denko Corporation

Land

🇯🇵 Japan