Process for producing 2-acylthiophene compound

C - Chemistry – Metallurgy – 07 – D

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C07D 333/22 (2006.01) A61K 31/381 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2544286

A process for producing a 2-acylthiophene compound reduced in the content of the 3-acyl isomer generated as a by-product. The process, which is for producing a 2-acylthiophene compound represented by the general formula (4): [Chemical formula 4] (4) (wherein R1 represents hydrogen, C1-6 alkyl, phenyl, or halogeno and R2 represents C1-6 alkyl or phenyl), is characterized by reacting a thiophene compound represented by the general formula (1): [Chemical formula 1] (1) (wherein R1 is the same as defined above) with at least one member selected from the group consisting of acid anhydrides represented by the general formula (2): [Chemical formula 2] (2) (wherein R2 is the same as defined above) and acid halides represented by the general formula (3): [Chemical formula 3] (3) (wherein R2 is the same as defined above and X represents halogeno) in the presence of a solid acid catalyst at a temperature lower than 75~C in the absence of any solvent.

L'invention concerne un procédé de production d'un composé de 2-acylthiophène dont le contenu d'isomère 3-acyle engendré en tant que sous-produit est amoindri. Ce procédé destiné à la production d'un composé de 2-acylthiophène représenté par la formule générale (4) (dans laquelle R?1¿ représente l'hydrogène, C¿1-6? alkyle, phényle ou halogène et R?2¿ représente C¿1-6 ?alkyle ou phényle) est caractérisé par la réaction d'un composé de thiophène représenté par la formule générale (1) (dans laquelle R?1¿ est tel que susmentionné) avec au moins un élément sélectionné parmi le groupe comprenant des anhydrides acides représentés par la formule générale (2) (dans laquelle R?2¿ est tel que susmentionné) et des halogénures acides représentés par la formule générale (3), où R?2¿ est tel que susmentionné et X représente halogène, en présence d'un catalyseur acide solide à une température inférieure à 75 ·C en l'absence de tout solvant.

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