NOVEL BENZOCYCLOALKENECARBOXYLIC ACID AND PROCESS FOR ITS PREPARATION

PCT No. PCT/CH91/00064 Sec. 371 Date Nov. 20, 1991 Sec. 102(e) Date Nov. 20, 1991 PCT Filed Mar. 19, 1991 PCT Pub. No. WO91/14671 PCT Pub. Date Oct. 3, 1991.The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula (I) in free form or in salt form, can...

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Bibliographic Details
Main Authors ANDREAS VON SPRECHER, HANSJUERG WETTER
Format Patent
LanguageEnglish
Published 27.11.1991
Edition5
Subjects
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Summary:PCT No. PCT/CH91/00064 Sec. 371 Date Nov. 20, 1991 Sec. 102(e) Date Nov. 20, 1991 PCT Filed Mar. 19, 1991 PCT Pub. No. WO91/14671 PCT Pub. Date Oct. 3, 1991.The novel (S)-4-(2-bromobenzoyl)-5-hydroxy-benzocyclobutene-1-carboxylic i.e. the compound of the formula (I) in free form or in salt form, can be used as active ingredient in pharmaceutical preparations and can be prepared by a novel process, which is characterized 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.
Bibliography:Application Number: ZA19910002262