INDUSTRIAL PRODUCTION OF QUINOLONE-CARBOXYLIC ACID AND ITS SYNTHETIC INTERMEDIATE

PROBLEM TO BE SOLVED: To industrially advantageously obtain the subject compound useful as an antibacterial agent by reacting a specific 3-aminopyrrolidine with an aldehyde or a ketone to obtain a Schiff's base, temporarily protecting, condens ing with a quinolone skeleton and deprotecting. SOL...

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Hauptverfasser:	IKEBE TSUGIO, TSURUTA MINEO, OE TAKANORI, OKUDA HIROBUMI
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM AGRICULTURE ANIMAL HUSBANDRY BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES CHEMISTRY FISHING FORESTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HUNTING HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEST REPELLANTS OR ATTRACTANTS PLANT GROWTH REGULATORS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS TRAPPING
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Beschreibung
Zusammenfassung:	PROBLEM TO BE SOLVED: To industrially advantageously obtain the subject compound useful as an antibacterial agent by reacting a specific 3-aminopyrrolidine with an aldehyde or a ketone to obtain a Schiff's base, temporarily protecting, condens ing with a quinolone skeleton and deprotecting. SOLUTION: The objective quinolone-carboxylic acid derivative expressed by formula V and useful as an antibacterial agent is readily obtained in high purity and a high yield by condensing 3-aminomethyl-3-fluoromethylpyrrolidine of formula I, its R-isomer or its S-isomer with an aldehyde or a ketone of formula II [R and R are each H, an alkyl or a (substituted) aryl], temporarily protecting amino group as a Schiff's base to obtain a compound of formula III, condensing the compound, its R-isomer or its S-isomer with a compound having a quinolone skeleton of formula IV [R is F or a (halogen-substituted) acyloxy; R is a halogen or methoxy; Hal is a halogen] and deprotecting.