Process for the preparation of fluoroquinolonecarboxylic acids
AssigneeBayer Aktiengesellschaft
InventorsNorbert Lui, Hans Panskus
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Abstract
Fluoroquinolonecarboxylic acids can be prepared by hydrolysis of the corresponding C1-C4-alkyl esters with addition of water, acetic acid, and sulfuric acid using a drastically reduced amount of sulfuric acid if, relative to 1 mol of C1-C4-alkyl fluoroquinolonecarboxylate, less than 30 g of sulfuric acid are employed, the reaction mixture is heated to reflux for 0.5 to 8 hours, then a mixture of acetic acid, C1-C4-alkyl acetate, C1-C4-alkyl alcohol, and optionally water is distilled off, and finally the fluoroquinolonecarboxylic acid prepared is isolated.
Claims10
A process for the preparation of fluoroquinolonecarboxylic acids by hydrolysis of the corresponding C1-C4-alkyl esters comprising
- (a) mixing water, acetic acid, and sulfuric acid with a C1-C4-alkyl fluoroquinolonecarboxylate, wherein less than 30 g of sulfuric acid per 1 mol of C1-C4-alkyl fluoroquinolonecarboxylate are employed,
- (b) heating the resultant reaction mixture at reflux for 0.5 to 8 hours,
- (c) distilling off a mixture of acetic acid, C1-C4-alkyl acetate, C1-C4-alkyl alcohol, and optionally water, and
- (d) isolating the resultant fluoroquinolonecarboxylic acid.
Dependencies are inferred from the claim text.