Process for production of...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 261/20 (2006.01) C07C 67/303 (2006.01) C07C 69/738 (2006.01) C07D 311/14 (2006.01) C07B 61/00 (2006.01)

Patent

CA 2643052

Disclosed is a production process using, as an intermediate, a 6-(halomethyl)-1,2-benzisooxazol-3(2H)-one derivative represented by the general formula: Wherein R5 represents a methyl group substituted by at least one phenyl group which may be substituted, or an oxygenated heterocyclic ring which may be substituted; and X represents a halogen atom. The process is useful for the production of 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)methoxy]phenyl]propionic acid, which is useful as an antirheumatic agent, in a high yield and in a safe and simple manner.

La présente invention concerne un procédé de production utilisant, en tant qu'intermédiaire, un dérivé de 6-(halométhyl)-1,2-benzisooxazol-3(2H)-one représenté par la formule générale : où R<SUP>5</SUP> représente un groupe méthyle substitué par au moins un groupe phényle pouvant être substitué, ou un cycle hétérocyclique oxygéné pouvant être substitué; et X représente un atome d'halogène. Le procédé est utile pour la production, avec un haut rendement et de manière sûre et simple, de l'acide 3-[5-[4-(cyclopentyloxy)-2-hydroxybenzoyl]-2-[(3-hydroxy-1,2-benzisoxazol-6-yl)méthoxy]phényl] propionique, lequel est utile en tant qu'agent antirhumatismal.

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