313340-08-8

Usage

Uses

3,5-Dichloro-6-ethyl-2-pyrazinecarboxamide acts as a reagent in the preparation of nitrogen-containing heterocyclic derivatives as remedies for complications of diabetes.

Upstream product

• 313339-92-3 3,5-dichloro-pyrazine-2-carbonitrile 
• 312736-50-8 3,5-dichloropyrazine-2-carboxamide 
• 1314936-02-1 3,5-dichloro-2-ethylpyrazine 
• 77287-34-4 formamide 
• 1254055-46-3 3,5-dichloro-6-ethylpyrazine-2-carbonitrile 

Downstream Products

• 1254048-03-7 5-{[(1-aminocyclohexyl)methyl]amino}-6-ethyl-3-{[3-(methylsulfonyl)phenyl]amino}pyrazine-2-carboxamide 
• 1254049-66-5 6-ethyl-5-[(1-methylpiperidin-3-yl)amino]-3-{[3-(methylsulfonyl)phenyl]amino}pyrazine-2-carboxamide 
• 1254055-46-3 3,5-dichloro-6-ethylpyrazine-2-carbonitrile 

Relevant academic research and scientific papers

Synthesis method of 3,5-dichloro-6-ethylpyrazineformamide

The invention discloses a synthetic method of 3,5-dichloro-6-ethylpyrazine formamide, and relates to the technical field of intermediate for synthesizing gilteritinib. The method is technically characterized by comprising the following steps: heating 2,6-dichloropyrazine and formamide to 70-130 DEG C, and carrying out free radical oxidation reaction under the action of persulfate to obtain 3,5-dichloropyrazine formamide; carrying out heating reflux on 3,5-dichloropyrazine formamide for 3-6 h under the action of a dehydrating agent, and synthesizing 3,5-dichloropyrazine formonitrile through dehydration; carrying out a Grignard reactionon the 3,5-dichloropyrazine formonitrile in an organic solvent A under the action of a methylation reagent to prepare 3,5-dichloro-2-acetylpyrazine; under theaction of an acidic catalyst and a silicon-hydrogen reducing agent, reducing the 3,5-dichloro-2-acetyl pyrazine in an organic solvent B to obtain 3,5-dichloro-2-ethyl pyrazine; and heating the 3,5-dichloro-2-ethyl pyrazine and formamide to 50-120 DEG C, and carrying out free radical oxidation reaction under the action of persulfate to obtain the 3,5-dichloro-6-ethylpyrazine formamide. According to the invention, the operation method is simple, the reaction conditions of the synthesis process are mild, the cost is reduced, and meanwhile high economic benefits can be brought.

Preparation method of Gilteritinib key intermediate

The invention relates to the field of drug synthesis, and particularly discloses a preparation method of a Gilteritinib key intermediate, namely a method for synthesizing a 3,5-dichloro-6-ethylpyrazinecarboxamide intermediate (compound I). The method is novel in route, simple and convenient to operate, high in yield, good in safety and suitable for industrial production, and comprises the following steps: by taking ethyl propionyl acetate as an initial raw material, carrying out hydrolytic acylation to obtain a compound III; carrying out ring closing on the compound III and aminomalononitrilep-toluenesulfonate to obtain a compound V; then carrying out amino diazotization chlorination to obtain a compound VI; carrying out phosphorus oxychloride transposition on the compound VI to obtain 3,5-dichloro-6-ethylpyrazine-2-carbonitrile (a compound VII); and hydrolyzing the compound VII to obtain the 3,5-dichloro-6-ethylpyrazinecarboxamide intermediate (compound I).