313340-08-8Relevant articles and documents
Preparation method of Gilteritinib key intermediate
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Paragraph 0022; 0030-0032; 0040-0041, (2020/07/28)
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).