Preparation method of 2-hydroxyethylaminocaproic acid ester compound and its application

The novel preparation method for 2-hydroxyethylaminocaproic acid ester compounds enhances mRNA delivery efficiency by addressing enzymatic degradation and cell membrane barriers, improving organ targeting and distribution.

JP2025531089APending Publication Date: 2025-09-19SUZHOU SUNCADIA BIOPHARM CO LTD +1
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Patent Information

Application Number
JP2025514138
Authority / Receiving Office
JP · JP
Patent Type
Applications
Current Assignee / Owner
Priority Date
2022-09-19
Filing Date
2023-09-19
Publication Date
2025-09-19

AI Technical Summary

Technical Problem

Current methods for delivering in vitro synthesized mRNA into cells face challenges such as enzymatic degradation and cell membrane barriers, and existing ionizable lipids for liposome-mediated nucleic acid delivery systems have limitations in organ targeting.

Method used

A novel method for preparing 2-hydroxyethylaminocaproic acid ester compounds by reacting specific compounds under reducing agent conditions, using sodium borohydride or sodium triacetoxyborohydride, and incorporating a base like N,N-diisopropylethylamine, to enhance the delivery efficiency and organ targeting of mRNA.

Benefits of technology

The prepared compounds improve the delivery efficiency of mRNA by overcoming enzymatic degradation and cell membrane barriers, achieving better distribution in target organs like the liver and reducing accumulation in the spleen.

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Abstract

The present disclosure relates to a method for preparing a 2-hydroxyethylaminocaproic acid ester compound and its application. Specifically, the present disclosure provides a method for preparing a compound of formula (I) or a salt thereof, the method comprising reacting a compound of formula (A) with a compound of formula (B) to form the compound of formula (I). The overall process is simple to operate, has high yields, and provides excellent sample quality, making it suitable for large-scale production. [Formula 1] JPEG2025531089000041.jpg31149
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