PRODUCTION OF QUINOLINECARBOXYLIC ACID ESTER DERIVATIVE

PROBLEM TO BE SOLVED: To obtain a compound useful as a synthetic intermediate for biologically active substance such as agrochemicals and medicines from an inexpensive and readily available raw material. SOLUTION: An acrylic acid ester of formula I (R is a 1-10C alkyl; R is a cycloalkyl which may be...

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Bibliographic Details
Main Authors WATANABE TSUNEO, UMETSU KAZUTO
Format Patent
LanguageEnglish
Published 02.12.1997
Edition6
Subjects
CHEMISTRY
HETEROCYCLIC COMPOUNDS
METALLURGY
ORGANIC CHEMISTRY
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Summary:PROBLEM TO BE SOLVED: To obtain a compound useful as a synthetic intermediate for biologically active substance such as agrochemicals and medicines from an inexpensive and readily available raw material. SOLUTION: An acrylic acid ester of formula I (R is a 1-10C alkyl; R is a cycloalkyl which may be substituted by a halogen; X is H, F, Cl, a 1-10C alkyl or a 1-10C alkoxy; X is H, F or Cl; X is H, an alkyl or nitro) is subjected to cyclization reaction by using an ester of formula II (R and R are each a 1-10C alkyl) as a solvent in the presence of a base (e.g. sodium hydride) at 20-150 deg.C to afford a compound of formula III. 1-Cyclopropyl-6,7- difluoro-1,4-dihydro-4-oxo-3-quinolincarboxylic acid ethyl ester is exemplified as the compound of formula III. Ethyl acetate, ethyl propionate, etc., is used as the solvent of formula II.
Bibliography:Application Number: JP19960127312