A method for synthesizing compound 2,4-dichloro-5-fluoro-6-methylpyrimidine

By optimizing raw materials and process parameters, a new 2,4-dichloro-5-fluoro-6-methylpyrimidine synthesis method is provided, which solves the problems of many by-products and low yields in the existing synthesis route, and achieves a high yield and low cost synthesis effect.

CN119751361APending Publication Date: 2025-04-04上海毕得医药科技股份有限公司
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Patent Information

Application Number
CN202411951996.4
Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
Filing Date
2024-12-27
Publication Date
2025-04-04

AI Technical Summary

Technical Problem

The existing synthesis route of 2,4-dichloro-5-fluoro-6-methylpyrimidine has the disadvantages of easy generation of by-products and low yields. New synthetic routes are needed to reduce by-products and improve production efficiency.

Method used

By optimizing raw materials and process parameters, a new synthesis method is provided, which involves mixing urea, organic solvent and alkali and adding ethyl 2-fluoroacetoacetate dropwise, then dropping into acetic acid to continue the reaction, and finally reacting with N,N-dimethylformamide and oxyphosphine trichloride to obtain 2,4-dichloro-5-fluoro-6-methylpyrimidine.

Benefits of technology

The high yield and low cost synthesis of the compound 2,4-dichloro-5-fluoro-6-methylpyrimidine is achieved, which is suitable for process amplification and reduces the generation of by-products.

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Abstract

The invention discloses a method for synthesizing a compound 2,4-dichloro-5-fluoro-6-methylpyrimidine, and belongs to the technical field of organic synthesis. The synthetic method of the present invention includes: mixing urea, organic solvent I and alkali, cooling, dropping ethyl 2-fluoroacetoacetate, stirring reaction, and obtaining a reaction solution; dropping the above-mentioned obtained reaction solution into the stirred acetic acid, dropping and completing the stirring reaction, post-processing, and obtaining 5-fluoro-6-methylpyrimidine-2,4 (1H, 3H)-dione; after mixing 5-fluoro-6-methylpyrimidine-2,4 (1H, 3H)-dione with organic solvent II, N, N-dimethylformamide and phosphorus oxychloride are successively added, reacted, post-processed, and spin-dried to obtain 2,4-dichloro-5-fluoro-6-methylpyrimidine. The present invention provides a method for synthesizing 2,4-dichloro-5-fluoro-6-methylpyrimidine at low cost, with an ideal yield of intermediate products and final products, and has the advantage of process amplification potential.
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Citation Information

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