Method for producing nucleic acid oligomer

By using fluoride ions with specific additives to deprotect triisopropylsilyloxymethyl-protected nucleic acid oligomers, the method enhances the purity of nucleic acid oligomers, addressing the purity issues in existing production methods.

WO2026048956A1 Publication Date: 2026-03-05SUMITOMO CHEM CO LTD
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Patent Information

Application Number
PCT/JP2025/030349
Authority / Receiving Office
WO · WO
Patent Type
Applications
Current Assignee / Owner
Priority Date
2024-08-29
Filing Date
2025-08-28
Publication Date
2026-03-05

AI Technical Summary

Technical Problem

The purity of nucleic acid oligomers produced using phosphoramidite compounds with a triisopropylsilyloxymethyl group protection at the 2'-position of ribose is not satisfactory.

Method used

Contacting nucleic acid oligomers with fluoride ions in the presence of specific additives to deprotect the triisopropylsilyloxymethyl group, using compounds like ammonia, methylamine, or nitrogen-containing heterocyclic compounds, to enhance the deprotection efficiency.

Benefits of technology

This method improves the purity of nucleic acid oligomers by effectively removing the triisopropylsilyloxymethyl group, leading to higher quality products.

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Abstract

The present invention provides an efficient method for producing a nucleic acid oligomer, in particular, the method for efficiently deprotecting a triisopropylsilyloxymethyl group of a ribose in which a hydroxyl group at a 2'-position in a nucleic acid oligomer has been protected by the triisopropylsilyloxymethyl group. Additionally, the present invention provides the method for producing a nucleic acid oligomer, the method including a step for contacting, with fluoride ions, in the presence of a specific additive, a nucleic acid oligomer that contains ribose having the hydroxyl group at the 2'-position protected by the triisopropylsilyloxymethyl group, to deprotect the triisopropylsilyloxymethyl group, wherein the additive is a compound, etc. represented by formula (A).
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