C - Chemistry – Metallurgy – 07 – C
Patent
C - Chemistry, Metallurgy
07
C
C07C 255/41 (2006.01) A61K 31/277 (2006.01) A61P 25/16 (2006.01) C07C 253/30 (2006.01)
Patent
CA 2674094
The present invention relates to a new process for preparing Entacapone substantially free of Z-isomer from 3, 4-dihydroxy-5-Nitrobenzaldehyde and N, N-Dimethylcyano acetamide, or directly from a mixture of (E) - and (Z) - isomers of Entacapone, by formation of organic or inorganic salts, specially piperidine and sodium ones. A new crystalline form G of Entacapone can be obtained from this method in a fast, efficient, and simple way and substantially free of Z-isomer. Another object of the invention is a pharmaceutical composition comprising it.
La présente invention concerne un procédé inédit de préparation d'entacapone essentiellement exempte d'isomère Z à partir de 3,4-dihydroxy-5-nitrobenzaldéhyde et de N,N-diméthylcyanoacétamide, ou directement à partir d'un mélange d'isomères E et Z d'entacapone, par formation de sels organiques ou inorganiques, en particulier de sels de pipéridine et de sodium. Une forme cristalline inédite G de l'entacapone, essentiellement exempte d'isomère Z, peut être obtenue grâce à ce procédé de façon rapide, efficace et simple. Un autre objet de la présente invention correspond à une composition pharmaceutique contenant ladite entacapone.
Benet-Buchholz Jordi
Molina Ponce Andres
Palomo Nicolau Francisco Eugenio
Sola Carandell Lluis
Chemo Iberica S.a.
Robic
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