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ES455333A1 - A PROCEDURE FOR THE PREPARATION OF 5-FLUOR-2-METHYL- (P-METHYLSULPHENYLBENZYLIDEN) -INDEN-3-ACETIC ACID OR ITS SALTS. - Google Patents

A PROCEDURE FOR THE PREPARATION OF 5-FLUOR-2-METHYL- (P-METHYLSULPHENYLBENZYLIDEN) -INDEN-3-ACETIC ACID OR ITS SALTS.

Info

Publication number
ES455333A1
ES455333A1 ES455333A ES455333A ES455333A1 ES 455333 A1 ES455333 A1 ES 455333A1 ES 455333 A ES455333 A ES 455333A ES 455333 A ES455333 A ES 455333A ES 455333 A1 ES455333 A1 ES 455333A1
Authority
ES
Spain
Prior art keywords
acetic acid
methyl
fluoro
methylsulphinyl
methylthio
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Expired
Application number
ES455333A
Other languages
Spanish (es)
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck and Co Inc
Original Assignee
Merck and Co Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority claimed from US426864A external-priority patent/US3870753A/en
Priority claimed from US05/486,031 external-priority patent/US3970693A/en
Priority claimed from US05/509,602 external-priority patent/US3944600A/en
Application filed by Merck and Co Inc filed Critical Merck and Co Inc
Publication of ES455333A1 publication Critical patent/ES455333A1/en
Expired legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C317/00Sulfones; Sulfoxides
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/455Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation with carboxylic acids or their derivatives
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/45Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by condensation
    • C07C45/46Friedel-Crafts reactions
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/65Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by splitting-off hydrogen atoms or functional groups; by hydrogenolysis of functional groups
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/65Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by splitting-off hydrogen atoms or functional groups; by hydrogenolysis of functional groups
    • C07C45/66Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by splitting-off hydrogen atoms or functional groups; by hydrogenolysis of functional groups by dehydration
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/673Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by change of size of the carbon skeleton
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C45/00Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
    • C07C45/61Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups
    • C07C45/67Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton
    • C07C45/68Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms
    • C07C45/72Preparation of compounds having >C = O groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds by reactions not involving the formation of >C = O groups by isomerisation; by change of size of the carbon skeleton by increase in the number of carbon atoms by reaction of compounds containing >C = O groups with the same or other compounds containing >C = O groups
    • C07C45/75Reactions with formaldehyde
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/587Unsaturated compounds containing a keto groups being part of a ring
    • C07C49/687Unsaturated compounds containing a keto groups being part of a ring containing halogen
    • C07C49/697Unsaturated compounds containing a keto groups being part of a ring containing halogen containing six-membered aromatic rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/80Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C49/00Ketones; Ketenes; Dimeric ketenes; Ketonic chelates
    • C07C49/76Ketones containing a keto group bound to a six-membered aromatic ring
    • C07C49/80Ketones containing a keto group bound to a six-membered aromatic ring containing halogen
    • C07C49/807Ketones containing a keto group bound to a six-membered aromatic ring containing halogen all halogen atoms bound to the ring
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/28Phosphorus compounds with one or more P—C bonds
    • C07F9/54Quaternary phosphonium compounds
    • C07F9/5456Arylalkanephosphonium compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

5-Fluoro-2-methyl-1-(p-methylsulphinylbenzylidene)indenyl-3-acetic acid or its salts are prepared. The said acid is obtained by condensing 5-fluoro-2-methyl-1-R1-benzylindene, where R1 is p-methylthio or p-methylsulphinyl, with glyoxylic acid, its salt or ester to give the corresponding 5-fluoro-2-methyl-1-(p-methylthio- (or methylsulphinyl)benzyl)indenylidene-3-acetic acid, its salt or ester. If R1 is p-methylsulphinyl, the indenylidene compound is isomerised to indenyl-3-acetic acid. If R1 denotes methylthio, then the resulting indenylidene-3-acetic acid is isomerised to 5-fluoro-2-methyl-1-(p-methylthiobenzylidene)indenyl-3-acetic acid and the p-methylthio radical is then oxidised to the p-methylsulphinyl group. However, the oxidation can also be carried out first and the isomerisation subsequently. The said compounds can be used as active agents in anti-inflammatory medicaments.
ES455333A 1973-12-20 1977-01-25 A PROCEDURE FOR THE PREPARATION OF 5-FLUOR-2-METHYL- (P-METHYLSULPHENYLBENZYLIDEN) -INDEN-3-ACETIC ACID OR ITS SALTS. Expired ES455333A1 (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US426864A US3870753A (en) 1973-12-20 1973-12-20 Process for preparing indenyl acetic acids
US05/486,031 US3970693A (en) 1974-07-05 1974-07-05 Process for preparing indene acetic acids
US05/509,602 US3944600A (en) 1973-12-20 1974-09-30 Indenylidene-3-acetic acid process for preparing indene acetic acids

Publications (1)

Publication Number Publication Date
ES455333A1 true ES455333A1 (en) 1978-05-01

Family

ID=27411527

Family Applications (2)

Application Number Title Priority Date Filing Date
ES432921A Expired ES432921A1 (en) 1973-12-20 1974-12-13 Indeneacetic acids
ES455333A Expired ES455333A1 (en) 1973-12-20 1977-01-25 A PROCEDURE FOR THE PREPARATION OF 5-FLUOR-2-METHYL- (P-METHYLSULPHENYLBENZYLIDEN) -INDEN-3-ACETIC ACID OR ITS SALTS.

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES432921A Expired ES432921A1 (en) 1973-12-20 1974-12-13 Indeneacetic acids

Country Status (16)

Country Link
JP (1) JPS5331153B2 (en)
AR (2) AR210484A1 (en)
CA (1) CA1044255A (en)
CH (1) CH616152A5 (en)
DD (1) DD116819A5 (en)
DE (1) DE2462380C2 (en)
DK (1) DK140835B (en)
ES (2) ES432921A1 (en)
FI (1) FI62287C (en)
FR (1) FR2255060B1 (en)
GB (1) GB1479519A (en)
IE (1) IE41529B1 (en)
NL (1) NL170534C (en)
NO (2) NO140857C (en)
SE (2) SE426818B (en)
YU (2) YU41017B (en)

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3732292A (en) * 1970-05-01 1973-05-08 Merck & Co Inc Indenyl compounds
US3822310A (en) * 1971-01-21 1974-07-02 Merck & Co Inc Substituted indenyl acetic acids
NL7200058A (en) * 1971-01-21 1972-07-25

Also Published As

Publication number Publication date
DK629674A (en) 1975-08-25
YU331674A (en) 1982-02-28
DK140835C (en) 1980-04-28
FI62287C (en) 1982-12-10
YU41017B (en) 1986-10-31
NO141892C (en) 1980-05-28
NL170534C (en) 1982-11-16
FR2255060B1 (en) 1978-07-21
NO140857B (en) 1979-08-20
JPS5095254A (en) 1975-07-29
DD116819A5 (en) 1975-12-12
FR2255060A1 (en) 1975-07-18
IE41529B1 (en) 1980-01-30
CH616152A5 (en) 1980-03-14
NO744395L (en) 1975-07-14
NL7415701A (en) 1975-06-24
AR210484A1 (en) 1977-08-15
AU7623674A (en) 1976-06-10
SE8107702L (en) 1981-12-22
NO141892B (en) 1980-02-18
DK140835B (en) 1979-11-26
NO140857C (en) 1979-11-28
AR206334A1 (en) 1976-07-15
JPS5331153B2 (en) 1978-08-31
SE426818B (en) 1983-02-14
DE2460292B2 (en) 1977-06-16
ES432921A1 (en) 1977-03-16
SE7415063L (en) 1975-06-23
GB1479519A (en) 1977-07-13
DE2462380A1 (en) 1977-02-10
YU55981A (en) 1982-06-30
DE2462380C2 (en) 1982-11-11
CA1044255A (en) 1978-12-12
SE440774B (en) 1985-08-19
NO790360L (en) 1975-06-23
NL170534B (en) 1982-06-16
FI348974A7 (en) 1975-06-21
DE2460292A1 (en) 1975-06-26
IE41529L (en) 1975-06-20
FI62287B (en) 1982-08-31

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