Method for preparing (2s)-1-¬ (2r,3s)-5- chloro-3-(2-...

Details Method for preparing (2s)-1-¬ (2r,3s)-5- chloro-3-(2-... Method for preparing (2s)-1-¬ (2r,3s)-5- chloro-3-(2-...

C - Chemistry, Metallurgy

07

D

C07D 403/06 (2006.01)

Patent

CA 2348676

The invention concerns a method for preparing (2s)-1-[(2r,3s)-5- chloro-3-(2- chlorophenyl) -1-(3,4-dimethoxy benzenesulphonyl) -3-hydroxy-2, 3-dihydro-1h- indole-2-carbonyl] pyrrolidine-2- carboxamide, its solvates and/or hydrates by cyclising reaction of (2S)-1-{ [ [4-chloro-2- (2-chlorobenzoyl) phenyl]-(3, 4- dimethoxybenzene sulphonyl)amino] acetyl}pyrrolidine -2-carboxamide. Said method is characterised in that it consists in cyclisation by an alkaline metal hydroxide in a polyethyleneglycol having an average molecular weight ranging between 200 and 600, mixed with water.

L'invention concerne un procédé de préparation du (2S)-1-[(2R,3S)-5- chloro-3-(2- chlorophényl) -1-(3,4-diméthoxy benzène sulfonyl) -3-hydroxy-2, 3-dihydro-1H- indole-2-carbonyl] pyrrolidine-2- carboxamide, de ses solvats et/ou hydrates par réaction de cyclisation du (2S)-1-{ [ [4-chloro-2- (2-chlorobenzoyl) phényl]-(3, 4-diméthoxybenzène sulfonyl)amino] acétyl}pyrrolidine -2-carboxamide caractérisé en ce qu'on effectue la cyclisation par un hydroxyde de métal alcalin dans un polyéthylèneglycol de poids moléculaire moyen compris entre 200 et 600, en mélange avec de l'eau.

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