Process for preparing N-substituted 1H-pyrazole-5-carboxylate compounds and derivatives thereof

摘要

The present invention relates to a process for preparing an N-substituted 1H-pyrazole-5-carboxylate compound of the formula (I-A);;comprising the steps of
i) deprotonating a compound of the formula (II);in which the variables R1, R2 and r are each as defined in the description and the claims,with a magnesium-organic base having a carbon bound magnesium; andii) subjecting the product obtained in step (i) to a carbonylation by reacting it with a reagent selected from the group consisting carbon dioxide or a carbon dioxide equivalent, to obtain a compound of formula (I-A);

and it relates to further conversions to yield a N-substituted 1H-pyrazole-5-carbonyl chloride compound of the formula (I)
;