Benzocycloalkenecarboxylic acid and process for it's...

C - Chemistry – Metallurgy – 07 – C

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C07C 51/64 (2006.01) A61K 31/19 (2006.01) C07B 57/00 (2006.01) C07C 51/487 (2006.01) C07C 62/38 (2006.01)

Patent

CA 2055602

4-18007/= Novel benzocycloalkenecarboxylic acid and process for its preparation Abstract The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula Image (I), in free form or in salt form, can be used as active ingredient in pharmaceuticalpreparations and can be prepared by a novel process, which is characterised in that racemic 4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is reacted at elevated temperature with at least the equimolar amount of quinine in an alcoholic solvent for from approximately 6 to approximately 48 hours, the quinine salt of the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid, precipitated in crystalline form as the direct reaction product, is separated from the reaction mixture, and the (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic acid is set free from this salt by acid treatment in a customary manner, and, if desired, this free acid is converted into a salt.

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