PREPARATION OF ISOXAZOLE-5-CARBOXYLIC ACID AMIDE DERIVATIVE

Process for the preparation of isoxazole-5-carboxamide derivatives III of the general formula I in which R is an aliphatic radical having 1 to 20, a cycloaliphatic radical having 3 to 10, an aromatic radical having 6 to 10, a heteroaromatic or heterocyclic radical having 3 to 10, or an araliphatic r...

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Hauptverfasser: NORUBERUTO GETSUTSU, TOOMASU KIYUKENHEENAA, BUORUFUGANGU FUROINTO, FUORUKAA MAIBUARUTO
Format: Patent
Sprache:eng
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Zusammenfassung:Process for the preparation of isoxazole-5-carboxamide derivatives III of the general formula I in which R is an aliphatic radical having 1 to 20, a cycloaliphatic radical having 3 to 10, an aromatic radical having 6 to 10, a heteroaromatic or heterocyclic radical having 3 to 10, or an araliphatic radical having 4 to 12, carbon atoms, it being possible for these radicals to be substituted by substituents which are inert under the reaction conditions, R is an alkyl group, and in which the radicals R and R are identical or different and represent hydrogen or C3- to C8-cycloalkyl groups which are unsubstituted or substituted by C1- to C6-alkyl, C1- to C6-cyanoalkyl, C2- to C6-alkenyl, C2- to C6-alkynyl and/or 1 to 3 C1- to C4-alkyl substituents, or linked to form a 5-8-membered cycloaliphatic ring which can contain a further nitrogen or an oxygen atom, with the proviso that, if R is the methyl group and R and R are a combination of hydrogen and the isopropyl group, then R is not an ethyl group, by reacting isoxazole-4,5-dicarboxylic acid diesters of the general formula II in which R is an alkyl group which is identical with, or different from, the alkyl group R , with an amine of the general formula III at temperatures from 0 to 100 DEG C.