Methods for isolating propargylated aminoindans

Details Methods for isolating propargylated aminoindans Methods for isolating propargylated aminoindans

C - Chemistry, Metallurgy

07

C

C07C 209/84 (2006.01)

Patent

CA 2630037

Disclosed is a process for isolating from a reaction mixture a salt of a mono- propargylated aminoindan having the structure (I) wherein R1 is H, hydroxyl, alkoxy or (II) wherein Y is 0 or S; R2 and R3 is each independently, C1-8 alkyl, C6-12 aryl, C6-12 aralkyl, each optionally halo substituted, or hydrogen ; where the reaction mixture further comprises a solven, a primary aminoindan having the structure (III) wherein R1 is defined as above, and a tertiary aminoindan having the structure (IV) the process comprising d) adding an acid to the reaction mixture; e) crystallizing the mono-propargylated aminoindan under conditions suitable for the formation of a crystalline salt of the mono-propargylated aminoindan ; and f) recovering the crystalline salt of the mono- propargylated aminoindan, wherein the process is performed without addition of an organic solvent. Also disclosed are the crystalline diastereomeric salts produced by the process and pharmaceutical compositions containing the salts.

L~invention concerne un procédé permettant d~isoler, à partir d~un mélange réactionnel, un sel d~un amino-indane monopropargylé de structure (I), dans laquelle R1 est un atome d~hydrogène, un hydroxyle, un alcoxy, ou (II), dans laquelle Y est un atome d~oxygène ou de soufre ; R2 et R3 sont chacun indépendamment un alkyle en C1-8, un aryle en C6-12 ou un aralkyle en C6-12, éventuellement substitués par un halogène, ou bien un atome d~hydrogène ; le mélange réactionnel contient en outre un solvant, un amino-indane primaire de structure (III) dans laquelle R1 est tel que défini précédemment, et un amino-indane tertiaire de structure (IV). Le procédé comprend les étapes consistant à : a) ajouter un acide au mélange réactionnel ; b) cristalliser l~amino-indane monopropargylé dans des conditions permettant la formation d~un de ses sels cristallins ; et c) récupérer le sel cristallin d~amino-indane monopropargylé, le procédé étant mis en AEuvre sans ajout de solvant organique. L~invention concerne également les sels diastéréoisomériques cristallins produits par le procédé, et des compositions pharmaceutiques contenant ces sels.

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