2-QUINOLONE DERIVATIVE

2-QUINOLONE DERIVATIVE

NEW MATERIAL:A 4-hydroxy-2-quinolone derivative of formula I [R -R are H, 1-8C alkyl, halogen, 1-5C alkoxyl, nitro, cyano, 1-3C halogenated alkyl or COOR (R is H or 1-3C alkyl) except when R -R are H at the same time] and a salt thereof. EXAMPLE:4-Hydroxy-3-(2,3,4-trimethoxybenzoyl)-2-quinolone. USE...

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Hauptverfasser: MURASE MASAO, INOUE YOSHIROU, ADACHI MASAHIRO, AOYANAGI YOSHIAKI, KOUNO TATSUHIKO, NOMURA CHIYUUKEI, JIYOUKAI SHIYOUICHI, ENOMOTO HIROSHI
Format: Patent
Sprache:eng
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Beschreibung
Zusammenfassung:NEW MATERIAL:A 4-hydroxy-2-quinolone derivative of formula I [R -R are H, 1-8C alkyl, halogen, 1-5C alkoxyl, nitro, cyano, 1-3C halogenated alkyl or COOR (R is H or 1-3C alkyl) except when R -R are H at the same time] and a salt thereof. EXAMPLE:4-Hydroxy-3-(2,3,4-trimethoxybenzoyl)-2-quinolone. USE:A medicine such as an antiallergic agent, antitussive and expectorant, remedy for asthma, etc., orally administrable, and having a prolonged duration of drug efficacy. The dose thereof is 1-100mg/day for the oral administration once - in divided three portions. PROCESS:A compound of formula II (R is lower alkyl) is subjected to the ring closing reaction in the presence of a base, e.g. a sodium alkoxide, in a suitable solvent under heating at 50-130 deg.C for 1-10hr to give the aimed compound of formula I .