A process for the preparation of vonomaci x fumarate

By carrying out the ammoniation reduction reaction of compound 3 at low temperature and directly forming a salt with fumaric acid, the problem of excessive impurity generation in the prior art was solved, and the preparation of vonoprazan fumaric acid with high purity and high yield was achieved, simplifying the operation and reducing the cost.

CN122356016APending Publication Date: 2026-07-10AOBO BIOMEDICAL TECHNOLOGY (HUBEI) CO LTD +1
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Patent Information

Application Number
CN202610297265.5
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Priority Date
2025-03-12
Filing Date
2026-03-12
Publication Date
2026-07-10

AI Technical Summary

Technical Problem

In the preparation of vonoprazan fumarate, the ammoniation-reduction reaction of compound 3 in the existing technology generates a large number of impurities that are difficult to remove through purification, affecting the purity and quality of the product. Furthermore, the existing methods increase the cost or complexity.

Method used

The reaction of compound 3 with a solution of methylamine alcohol and a reducing agent was carried out at low temperature, followed by quenching the reaction with an aqueous solution of acid, and then directly forming a salt with fumaric acid to generate vonorazan fumarate, thus avoiding intermediate steps and the use of additional reagents.

Benefits of technology

It effectively removed impurities A and D, reduced the content of impurity C, simplified the operation process, improved product yield and purity, and reduced production costs.

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Abstract

This invention belongs to the field of pharmaceutical technology and relates to a method for preparing vonoprazan fumarate. Compound 3 reacts with a methylamine alcohol solution and a reducing agent at low temperature, followed by quenching, and then forms a salt with fumaric acid to generate vonoprazan fumarate. In this method, the amination-reduction step is performed under mild conditions, and the product can be directly obtained by salt formation with fumaric acid after simple post-treatment following quenching, without the need for pre-preparing other intermediate salts. This method is simple to operate, low in cost, and yields a product with few impurities, making it suitable for industrial production.
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Citation Information

Patent Citations

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  • A method for preparing low-impurity vonoprazan fumarate

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  • Preparation method of vonoprazan fumarate

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