Vanillin and application of isomer thereof to preparation of NA inhibitor

The invention relates to 2-(2-benzyl hydrazono)-5-acyl-thiazole containing hydroxyl and methoxyl as well as pharmaceutically-acceptable salt, a pharmaceutical composition and application of the 2-(2-benzyl hydrazono)-5-acyl-thiazole in preparation of an influenza virus neuraminidase inhibitor, where...

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Hauptverfasser: HU AIXI, XIE WENXUE, NIE JIANXIA, WEI XIAOQIAN
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention relates to 2-(2-benzyl hydrazono)-5-acyl-thiazole containing hydroxyl and methoxyl as well as pharmaceutically-acceptable salt, a pharmaceutical composition and application of the 2-(2-benzyl hydrazono)-5-acyl-thiazole in preparation of an influenza virus neuraminidase inhibitor, wherein the 2-(2-benzyl hydrazono)-5-acyl-thiazole shown in a formula (1) is built based on vanillin andan isomer of the vanillin. By adopting the vanillin and an isomer of the vanillin as raw materials, 2-(2-benzyl hydrazono)-5-acyl-thiazole containing hydroxyl and methoxyl is prepared: the formula (1)is shown in the description, wherein R is selected from methyl, ethyl and C3 to C4 straight chain or C3 to C4 branch chain alkyl; R1 is selected from hydrogen, C1 to C2 alkyl, C3 to C4 straight chainor C3 to C4 branch alkyl, methyl fluoride, difluoromethyl, trifluoromethyl, bromomethyl, dibromomethyl, tribromomethyl, chloromethyl, dichloromethyl or trichloromethyl; Y is equal to 2-hydroxyl-3-methoxyl, 2-hydroxyl-4-methoxy