Process for the preparation of pyridylcarboxylic amides and...

C - Chemistry – Metallurgy – 07 – D

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C07D 213/81 (2006.01) C07D 213/79 (2006.01)

Patent

CA 2626465

The invention relates to a process for the preparation of pyridylcarboxylic amides and esters I, Formula (I) wherein Hal, X and R1 have the meanings given in claim 1, which comprises the following steps: (a) heating a mixture consisting essentially of trichloromethylpyridine II, Formula (II), wherein Hal has the meaning given, and 1.0 to 1.5 equivalents of concentrated sulfuric acid, characterized in that the trichloromethylpyridine II in a liquid form is added to the concentrated sulfuric acid at a temperature from 110~C to 160~C; and (b) reacting the intermediate product obtained in step (a) with an amine or alcohol III, HXR1, wherein X and R1 have the meaning given, optionally in the presence of a solvent and/or a base.

L'invention concerne un procédé pour la préparation d'amides et esters pyridylcarboxyliques de formule (I), selon laquelle Hal, X et R1 ont les significations données dans la revendication 1, lequel comprend les étapes suivantes : (a) une étape consistant à chauffer un mélange constitué essentiellement de trichlorométhylpyridine de formule (II), selon laquelle Hal a la signification donnée dans la revendication 1, et de 1,0 à 1,5 équivalent d'acide sulfurique concentré, caractérisé en ce qu'on ajoute la trichlorométhylpyridine II sous une forme liquide à l'acide sulfurique concentré à une température allant de 110°C à 160°C ; et (b) une étape consistant à faire réagir le produit intermédiaire obtenu dans l'étape (a) avec une amine ou un alcool de formule (III), selon laquelle X et R1 ont les significations données dans la revendication 1, éventuellement en présence d'un solvant et/ou d'une base.

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