Method for preparing trifluorobenzene pyrimidine

By using 2-aminopyridine and pyrimidine-5-formaldehyde as starting substrates in the trifluorophenylpyrimidine synthesis process, Schiff base condensation, reducing amination and cyclization reactions, many problems in the existing process were solved, and an efficient, economical and environmentally friendly synthesis process was achieved.

CN119707965APending Publication Date: 2025-03-28EAST CHINA UNIV OF SCI & TECH
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Patent Information

Application Number
CN202411917438.6
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-24
Publication Date
2025-03-28

AI Technical Summary

Technical Problem

There are many problems in the synthesis process of existing trifluorophenylpyrimidine, including the inappropriate storage of 2-(3-trifluoromethylphenyl)malonic chloride, low conversion rate of temperature-sensitive cyclization reaction, strict anhydrous requirements for Schiff base reaction, environmentally hazardous chloroform solvent use, high cost of sodium borohydride and complex post-treatment process.

Method used

Trifluorophenylpyrimidine was used as starting substrates, and trifluorophenylpyrimidine was produced by performing Schiff base condensation, reduction amination and cyclization reaction in an organic solvent. This method uses a water detacher instead of the water separation method, reducing reaction temperature and operational complexity, and improving reaction efficiency and purity through metal palladium catalysts.

Benefits of technology

It realizes an efficient, economical and environmentally friendly trifluorophenylpyrimidine synthesis process, reduces production costs and waste output, simplifies the post-treatment process, and improves yield and product purity.

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Abstract

The invention belongs to the field of pesticide intermediates and product preparation, and particularly relates to a method for preparing trifluorobenzene pyrimidine. The method disclosed by the invention comprises the following steps: (1) in a first organic solvent, carrying out Schiff base condensation reaction on 2-aminopyridine and pyrimidine-5-formaldehyde under the action of a first moisture scavenger to generate N-2-pyridine-5-pyrimidine methylenimine; (2) in a second organic solvent, carrying out reductive amination reaction on the N-2-pyridine-5-pyrimidine methylenimine and hydrogen under the action of a catalyst to generate N-2-pyridine-5-pyrimidine methylamine; and (3) in a third organic solvent, carrying out cyclization reaction on the N-2-pyridine-5-pyrimidine methylamine and 2-(3-trifluoromethylphenyl) malonyl chloride in the presence of an acid-binding agent, so as to prepare the trifluorobenzene pyrimidine. According to the method disclosed by the invention, the post-treatment operation times and the reaction reagent consumption are greatly reduced, and efficient and green production is realized.
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