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 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.