Method for producing oligonucleotide

The use of a deblocking solution with specific bases and solvents in solid-phase oligonucleotide synthesis addresses the issue of 2',3' rearrangement by-products, resulting in more efficient production of oligonucleotides.

WO2025229953A1 Publication Date: 2025-11-06SUMITOMO CHEM CO LTD
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Patent Information

Application Number
PCT/JP2025/016225
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-04-30
Filing Date
2025-04-28
Publication Date
2025-11-06

AI Technical Summary

Technical Problem

Existing methods for producing oligonucleotides through solid-phase synthesis face challenges in efficiently removing hydroxyl-protecting groups without producing undesirable 2',3' rearrangement by-products, which are common in both DNA and RNA synthesis.

Method used

A deblocking solution containing a base, an acid, and an aprotic solvent is used to efficiently remove the hydroxyl-protecting group at the chain extension terminal of oligonucleotides, where the base has a conjugate acid with an acid dissociation constant (pKa) of 5 or more and 12 or less, effectively suppressing the production of 2',3' rearrangement by-products.

Benefits of technology

This method allows for the efficient production of oligonucleotides with a reduced content of 2',3' rearrangement by-products, enhancing the overall synthesis efficiency.

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Abstract

The purpose of the present invention is to provide a method for efficiently producing an oligonucleotide by a solid-phase synthesis approach. The present invention provides a method for producing an oligonucleotide by a solid phase synthesis approach, the method comprising a step for reacting an oligonucleotide in which a hydroxyl group at a chain extendable end is protected with a protective group that can be removed under acidic conditions and a deblocking solution to remove a protective group for a hydroxyl group at the chain extendable end, wherein the deblocking solution is a deblocking solution containing a base, an acid, and an aprotic solvent, and the base is a base having an acid dissociation constant (pKa) of a conjugate acid of 5-12, and an oligonucleotide in which the content ratio of the 2', 3'transfer body is a certain amount or less.
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