A process for the preparation of polymorph form i of...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01)

Patent

CA 2640242

The invention relates to a process for the preparation of the pharmaceutically applicable polymorph Form I of (S)-(+)-methyl-.alpha.-(2-clorophenyl)-6,7- dyhidro-thieno¢3,2-c!-pyridine-5(4H)-acetate hydrogen sulfate of formula I; by reacting (S)-(+)-methyl-.alpha.-(2-chlorophenyl)-6,7-dyhidro-thieno¢3,2- c!pyridine-5(4H)-acetate and sulfuric acid in the presence of solvents which comprises dissolving (S)-(+)-methyl-.alpha.-(2-chloropnenyl)-6,7-dyhidro- thieno¢3,2-c!pyridine-5(4H)-acetate in an ether; mixing this solution with a solution of a C6-C11 alcohol and sulfuric acid; and recovering the so obtained compound of formula I from the mother liquor.

La présente invention concerne un procédé de synthèse de la forme polymorphique I de qualité pharmaceutique de l'hydrogénosulfate de (S)-(+)-méthyl-.alpha.-(2-chlorophényl)-6,7-dihydro-thiéno[3,2-c]-pyridine-5(4H)-acétate de formule I ; par réaction de (S)-(+)-méthyl-.alpha.-(2-chlorophényl)-6,7-dihydro-thiéno[3,2-c]pyridine-5(4H)-acétate et d'acide sulfurique en présence de solvants, ladite réaction comprenant la dissolution du (S)-(+)-méthyl-.alpha.-(2-chlorophényl)-6,7-dihydro-thiéno[3,2-c]pyridine-5(4H)-acétate dans un éther ; mélange de cette solution à une solution d'un alcool en C6-C11 et d'acide sulfurique ; et récupération du composé de formule I ainsi obtenu depuis la solution mère.

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