PROCESS FOR THE HYDROLYSIS OF QUINOLONE CARBOXYLIC ESTERS

Quinolone carboxylic esters of general formula (II) are hydrolyzed to form quinolone carboxylic acids of general formula (I): the method comprises the step A): A) reacting compounds of formula (II) with a mixture that comprises acetic acid, sulfuric acid and water. In step A), ≥ 30 to ≤ 40 mol a...

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Hauptverfasser: DIETZEL Antje, FEY Peter, WISCHNAT Ralf, LONGERICH Markus, BERWE Mathias, WIRTHS Jörg
Format: Patent
Sprache:eng ; spa
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Zusammenfassung:Quinolone carboxylic esters of general formula (II) are hydrolyzed to form quinolone carboxylic acids of general formula (I): the method comprises the step A): A) reacting compounds of formula (II) with a mixture that comprises acetic acid, sulfuric acid and water. In step A), ≥ 30 to ≤ 40 mol acetic acid, ≥ 0.3 to ≤ 1 mol sulfuric acid and ≥ 0.9 to ≤ 2.5 mol water are used per mol of compounds of formula (II). The process according to the invention is particularly suitable for the synthesis of the intermediate (I) in the synthesis of pradofloxacin. Los ésteres del ácido carboxílico de quinolona la fórmula general (II) se hidrolizan para dar ácidos quinoloncarboxílicos la fórmula general (I): (ver Fórmulas) El procedimiento comprende la etapa A): A) Reacción de compuestos de fórmula (II) con una mezcla que contiene ácido acético, ácido sulfúrico y agua En la etapa A) se utilizan por mol compuestos de la fórmula (II) = 30 a = 40 mol de ácido acético, = 0.3 a = 1 mol de ácido sulfúrico y = 0,9 a = 2.5 mol de agua. El procedimiento es particularmente adecuado para la síntesis del intermedio (I) en la síntesis de pradofloxacina.