- Preparation method of Gilteritinib key intermediate
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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).
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Paragraph 0022; 0028-0029; 0032; 0038-0039
(2020/07/28)
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- DIAMINO HETEROCYCLIC CARBOXAMIDE COMPOUND
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Provided is a compound useful as an inhibitor against the kinase activity of EML4-ALK fusion protein. As a result of intensive and extensive studies on compounds having inhibitory activity against the kinase activity of EML4-ALK fusion protein, the present inventors found that the diamino heterocyclic carboxamide compounds of the present invention had inhibitory activity against the kinase activity of EML4-ALK fusion protein. By this finding, the present invention was completed. The compounds of the present invention can be used as a pharmaceutical composition for preventing and/or treating cancer, such as lung cancer, non-small cell lung cancer, and small cell lung cancer.
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Page/Page column 22
(2012/03/08)
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