PRODUCTION OF PHENYLMALONIC ACID MONOANILIDE DERIVATIVE AND 3-PHENYL-2-QUINOLONE DERIVATIVE

NEW MATERIAL:The compound of formula I (X and Y are H or 1-3C alkoxy; Z is 1-3C alkoxy). EXAMPLE:2-(3-Methoxy-phenylcarbamoyl)-2-(2,4-dimethoxyphenyl)acetic acid. USE:Useful as a drug or its synthetic intermediate. PREPARATION:The compound of formula I is produced by reacting an aniline derivative o...

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Hauptverfasser: HIRATA KAZUMITSU, KAMIJO TETSUKIYO, TSUBAKI ATSUSHI, YAMAGUCHI TOSHIAKI
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creator HIRATA KAZUMITSU
KAMIJO TETSUKIYO
TSUBAKI ATSUSHI
YAMAGUCHI TOSHIAKI
description NEW MATERIAL:The compound of formula I (X and Y are H or 1-3C alkoxy; Z is 1-3C alkoxy). EXAMPLE:2-(3-Methoxy-phenylcarbamoyl)-2-(2,4-dimethoxyphenyl)acetic acid. USE:Useful as a drug or its synthetic intermediate. PREPARATION:The compound of formula I is produced by reacting an aniline derivative of formula II with a phenylmalonic acid monoester derivative of formula III (R is lower alkyl) in the presence of a dehydrative condensation agent (e.g. trimethylsilyl phosphite) at room temperature and removing the ester group of the product. Cyclization of the compound of formula I in the presence of a condensation agent gives a 3-phenyl-2-quinolone derivative of formula IV exhibiting osteogenesis promoting action and useful as a remedy for osteoporosis.
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
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
title PRODUCTION OF PHENYLMALONIC ACID MONOANILIDE DERIVATIVE AND 3-PHENYL-2-QUINOLONE DERIVATIVE
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