Synthetic method of 2-chlorine-5-fluorine-6-ethylpyrimidin-2-amine

A technique for the synthesis of ethylpyrimidine and its synthesis method, which is applied in the synthesis of 2-chloro-5-fluoro-6-ethylpyrimidine and the synthesis of pyrimidine derivatives, and can solve the problems of long synthetic routes, environmental pollution, and low yields , to avoid pollution, improve safety and reduce costs
CN110372603AInactive Publication Date: 2019-10-25南京普锐达医药科技有限公司
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
南京普锐达医药科技有限公司
Publication Date
2019-10-25
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthetic method of 2-chlorine-5-fluorine-6-ethylpyrimidin-2-amine. Step 1, sodium methoxide is dissolved in methyl alcohol, the temperature is lowered to the room temperature, carbamide is added, stirring is conducted after addition at the room temperature, 2-ethyl fluoropropioacetate is dropwise added, then the temperature is risen to reflux reaction for 2-3 hours, anda midbody A is obtained through purification; step 2, the midbody A, phosphorus oxychloride and organic alkali are mixed by weight ratio of 1 to 5-10 to 0.3-2, chlorination is conducted for 2-5 hoursat 25-100 DEG C, the mixture is cooled and subjected to vacuum concentration, extra phosphorus oxychloride is removed, after water is added for quenching, an organic solvent is used for extraction, drying and concentration are conducted, and then an intermediate product B is obtained; and step 3, ethyl alcohol, zinc powder and acetic acid are added in the intermediate product B, heating reflux reaction is conducted for 10-16 hours, the temperature is lowered, filtering is conducted, ethyl alcohol is removed by steaming, extraction is conducted through the organic solvent, a crude product is obtained through evaporation to dryness, and a pure product C is obtained through rectification under vacuum. According to the synthetic method of the 2-chlorine-5-fluorine-6-ethylpyrimidin-2-amine, theyield is increased, the reaction time is shortened, meanwhile the cost is lowered, and pollution on the environment is reduced.
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Description

technical field

[0001] The invention relates to a method for synthesizing pyrimidine derivatives, in particular to a method for synthesizing 2-chloro-5-fluoro-6-ethylpyrimidine, and belongs to the technical field of pharmaceutical intermediate synthesis. Background technique

[0002] Pyrimidine ring is one of the most common heterocycles in drugs and natural products. Pyrimidine heterocyclic compounds, as intermediates for the synthesis of such drugs, have important applications in the field of medicine, and are widely used in the research and development and clinical applications of anti-cancer drugs, anti-AIDS drugs, etc. Therefore, it is of great significance to develop and optimize the preparation process of such compounds.

[0003] The main problems of the synthesis method of 2-chloro-5-fluoro-6-ethylpyrimidine in the prior art are: long synthesis route, low yield, high toxicity of raw materials and environmental pollution. SUMMARY OF THE INVENTION

[0004] In order...

Claims

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