| 摘要 |
A process for the preparation of aminopyrazolecarboxylic acid derivatives of the general formula I <IMAGE> in which X denotes a -CN group or a -CO-R<3> group, R<1> denotes an alkyl group having 1 to 4 carbon atoms, R<2> denotes a hydrogen atom or an alkyl group having 1 to 4 carbon atoms, R<3> denotes an -OH group, an -O-R<4> group, an -NH2 group, an -NH(R<5>) group, an -N(R<5>)R<6> group, a phenyl group or a 2-thienyl group, R<4> denotes an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group, a benzyl group or an equivalent of a cation of an inorganic or organic base, R<5> denotes an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group or a benzyl group, R<6> has one of the meanings of R<5>, or R<5> and R<6> together, including the nitrogen atom to which they are bonded, denote an optionally substituted non-aromatic heterocyclic radical, is characterised in that a substituted hydrazine of the general formula II NC-CH(R<2>)-NH-N(R<1>)-CH2-Y (II> in which Y denotes a -CN group or a -CO-R<7> group, R<7> denotes an -O-R<8> group, an -N(R<5>)R<6> group, a phenyl group or a 2-thienyl group, R<8> denotes an alkyl group having 1 to 7 carbon atoms, a cycloalkyl group having 3 to 6 carbon atoms, a phenyl group or a benzyl group, and R<1>, R<2>, R<5> and R<6> have the above meaning, is dehydrogenated and the hydrazone obtained, of the general formula III NC-C(R<2>)=N-N(R<1>)-CH2-Y (III> in which R<1>, R<2> and Y have the above meaning, is cyclised and the reaction product obtained is optionally then hydrolysed and/or converted into the salts of the acids. The hydrazones III are novel compounds and, like the aminopyrazolecarboxylic acid derivatives I, are intermediates for the preparation of pharmaceutical active compounds.
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