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1. (EP0990637) PROCESS FOR PRODUCING KETOPROFEN AND 5-BENZOYL-3-METHYL-2-INDOLINONE

Office : European Patent Office
Application Number: 98917708 Application Date: 28.04.1998
Publication Number: 0990637 Publication Date: 05.04.2000
Publication Kind : A4
Prior PCT appl.: Application Number:JP1998001939 ; Publication Number: Click to see the data
IPC:
C 07B
C 07C
C 07C
C07D 209/34
C 07C
C 07D
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
B
GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
61
Other general methods
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
51
Preparation of carboxylic acids or their salts, halides, or anhydrides
06
from carboxylic acid amides
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
59
Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
40
Unsaturated compounds
76
containing keto groups
84
containing six-membered aromatic rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
30
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
32
Oxygen atoms
34
in position 2
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
51
Preparation of carboxylic acids or their salts, halides, or anhydrides
347
by reactions not involving formation of carboxyl groups
377
by splitting-off hydrogen or functional groups; by hydrogenolysis of functional groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
209
Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
02
condensed with one carbocyclic ring
04
Indoles; Hydrogenated indoles
30
with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to carbon atoms of the hetero ring
32
Oxygen atoms
34
in position 2
CPC:
C07D 209/34
Applicants: MEDICAL INFORMATION SERVICES I
Inventors: KONDO HISAO
HIGASHIKAWA TETSURO
KUBO AKINARI
SAITO NAOKI
Priority Data: 11123697 28.04.1997 JP
20927897 04.08.1997 JP
9801939 28.04.1998 JP
Title: (DE) VERFAHREN ZUR HERSTELLUNG VON KETOPROFEN UND 5-BENZOYL-3-METHYL-2-INDOLINON
(EN) PROCESS FOR PRODUCING KETOPROFEN AND 5-BENZOYL-3-METHYL-2-INDOLINONE
(FR) PROCEDE SERVANT A PREPARER KETOPROFENE ET 5-BENZOYLE-3-METHYLE-2-INDOLINONE
Abstract: front page image
(EN) The present invention relates to a process for producing ketoprofen, comprising the steps of: benzoylating 3-methyl-2-indolinone with benzoyl halide to yield 5-benzoyl-3-methyl-2-indolinone; cleaving an amido linkage that forms the 5-menbered ring moiety of 5-benzoyl-3-methyl-2-indolinone, with a basic compound; and substituting an amino group attached to an aromatic ring of the resulting compound by a hydrogen atom to yield the ketoprofen. By employing the process, it is possible to produce ketoprofen by ordinary steps without the need for use of any extremely poisonous chemical such as prussic acid compounds or any hard-to-handle chemical such as liquid ammonium, by more shortened steps as a whole, with an excellent yield.
(FR) Procédé servant à préparer kétoprofène par benzoylation de 3-méthyle-2-indolinone avec un halogénure de benzoyle, par clivage de la liaison amido constituant la fraction de noyau à cinq éléments de 5-benzoyle-3-méthyle-2-indolinone obtenue avec un composé basique et par remplacement d'un groupe amino aromatique du composé obtenu par un atome d'hydrogène. On peut obtenir un rendement très important de kétoprofène par l'intermédiaire d'étapes ordinaires, courtes dans leur ensemble, sans utiliser de produits chimiques présentant une toxicité extrêmement élevée, tels que des cyanures, ou des produits chimiques peu maniables, tels que de l'ammoniac liquide.
Also published as:
KR1020010012131JP3347745CN1253543CA2288125WO/1998/049127