A method for synthesizing 5-bromopyrimidine-4-carboxylic acid

The improved synthesis method of 5-bromopyrimidine-4-carboxylic acid, employing a mild two-step reaction process, solves the problems of low yield, high impurities, high cost, and high safety risks in existing technologies, and achieves industrial production with high yield and high purity.

CN122145396BActive Publication Date: 2026-07-24SHANDONG BAIQI BIOLOGICAL MEDICINE CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Patents(China)
Current Assignee / Owner
SHANDONG BAIQI BIOLOGICAL MEDICINE CO LTD
Filing Date
2026-05-11
Publication Date
2026-07-24

AI Technical Summary

Technical Problem

Existing methods for synthesizing 5-bromopyrimidine-4-carboxylic acid suffer from low yields, numerous impurities, difficult purification, high costs, and safety risks, making it difficult to meet the needs of industrial production.

Method used

5-Bromopyrimidine-4-carboxylic acid was prepared by a two-step reaction using methyl 4-hydroxypyrimidine-6-carboxylate as the starting material. N,N-dimethylformamide was used as the solvent, and N-bromosuccinimide and thionyl chloride were added in batches. Subsequently, the mixture was reacted with hydrazine hydrate, sodium hydroxide, and sodium hypochlorite. Finally, the mixture was treated with sodium thiosulfate. The temperature was controlled at 0~30℃ to avoid harsh conditions and hazardous reagents.

Benefits of technology

It improves the yield of intermediates and products, simplifies the purification process, reduces costs and safety risks, and is suitable for industrial production.

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Abstract

The application belongs to the technical field of medicine synthesis, and particularly relates to a synthesis method of 5-bromopyrimidine-4-carboxylic acid. 4-hydroxypyrimidine-6-methyl ester is used as a starting material, 5-bromo-4-hydroxypyrimidine-6-methyl ester is obtained through a bromination reaction, and then 5-bromopyrimidine-4-carboxylic acid is obtained through hydroxyl chlorination and hydrolysis dehalogenation. In the application, the problems of many by-products and great separation difficulty in the traditional synthesis process are avoided. Through accurate control of reaction conditions in each step, the reaction selectivity and product yield are effectively improved, the purity of the target product can reach more than 98%, the raw materials are easy to obtain and low in cost, the reaction conditions are mild and easy to operate, no special and expensive equipment is needed, the safety is high, the application is friendly to the environment, and the industrialized production can be easily realized.
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