FI113654B - Förfarande för framställning av terapeutiskt användbara azabicyklo[2.2.2]oktan-3-aminer - Google Patents

Förfarande för framställning av terapeutiskt användbara azabicyklo[2.2.2]oktan-3-aminer Download PDF

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Publication number
FI113654B
FI113654B FI925443A FI925443A FI113654B FI 113654 B FI113654 B FI 113654B FI 925443 A FI925443 A FI 925443A FI 925443 A FI925443 A FI 925443A FI 113654 B FI113654 B FI 113654B
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Prior art keywords
formula
compound
azabicyclo
methoxyphenyl
amine
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FI925443A
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English (en)
Finnish (fi)
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FI925443A0 (fi
FI925443A (fi
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Iii John A Lowe
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Pfizer
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D453/00—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids
    • C07D453/02—Heterocyclic compounds containing quinuclidine or iso-quinuclidine ring systems, e.g. quinine alkaloids containing not further condensed quinuclidine ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00—Drugs for disorders of the respiratory system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/20—Hypnotics; Sedatives
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Anesthesiology (AREA)
  • Pulmonology (AREA)
  • Dermatology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pyrrole Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Claims (8)

1. Förfarande för framställning av terapeutiskt an-vändbara azabicyklo [2.2.2]oktan-3-aminer med formeln •'-€c 5 väri R1 är väte eller Ci-6-alkyl; R2 är fenyl, pyridyl, tie-nyl eller furyl, och vilka grupper kan vara substituerade med 1-3 substituenter valda bland: Ci-4-alkyl, Ci-4-alkox-yl, klor, fluor, brom, jod och/eller trifluormetyl; och R3 10 är fenyl, naftyl, pyridyl, tienyl eller furyl, och vilka grupper kan vara substituerade med 1-3 substituenter valda bland: Ci_4-alkyl, Ci-4-alkoxyl, klor, fluor, brom, jod och/eller trifluormetyl; samt farmaceutiskt godtagbara sal-ter av dessa föreningar, kännetecknat av att man (a) 15 omsätter en förening med formeln R1--/ V ! « ;· väri R1 och R3 är säsom ovan definierats, med en förening • » · med formeln R2CH2NH2; (b) reducerar produkten frän denna re- : aktion; och (c) valfritt omvandlar föreningen med formeln * I · : 20 (I), vilken erhällits i steget (b) , tili ett f armaceutiskt ► · i godtagbart sait.
2. Förfarande enligt patentkrav 1, känneteck- , nat av att nämnda förening med formeln (V) erhälls genom * · ·; i att man med hjälp av en lösande metal1 reducerar en före- ’···* 25 ning med formeln (IV) • > « i i » | » » 113654 0/0 f IV H ♦ r3 I X" AA väri R1 och R3 är säsom definierats i patentkrav 1, och X" är en bromidjon, vätekarbonatjon eller nägon annan anjon, vilken alstrats under omsättningen av en förening raotsva-5 rande formeln R3 ?! R>__ Hl AA Va med brom och en svag oorganisk bas. ·’ 3. Förfarande enligt patentkrav 1, känneteck- , nat av att nämnda förening med formeln (V) erhälls genom ·' 10 att man med hjälp av väte sönderdelar en förening med for- : : meln :: 'ACA,, ,v N* K ;· \ x- aa väri R1, R3 och X' är säsom definierats i patentkrav 1.
1 I » · i · * t 113654
4. Förf arande enligt patentkrav 2, känneteck-n a t av att man oxiderar produkten frän den lösande metal lreduktionen, innan den omsätts med nämnda förening med formeln R2CH2NH2, för omvandlande av en förening med formeln . OH r1--) N + r3 X" ^ I 5 väri R1, R3 och X' är säsom definierats i patentkrav 1, till motsvarande förening med formeln (IV), definierad i patentkrav 2 .
5. Förf arande enligt patentkrav 3, känneteck-10 nat av att man oxiderar produkten fran nämnda hydrogeno- lys innan den omsätts med nämnda förening med formeln R2CH2NH2, för omvandlande av en förening med formeln OH R1--) . I X- » 1 · t | • väri R1 är väte eller Ci-4-alkyl; R3 är fenyl, naftyl, pyri- ; *· 15 dyl, tienyl eller furyl, vilka grupper kan vara substitue- : rade med 1-3 substituenter valda bland: Ci-4-alkyl, Ci-4- alkoxyl, klor, fluor, brom, jod och/eller trifluormetyl, !. och X’ är en bromidjon, vätekarbonatjon eller nägon annan ,- ·. anjon, vilken alstrats under omsättningen av en förening * · ·’ 2 0 med formeln * * t I · * · » » I I 113654 R3 R1__ III med brom och en svag oorganisk bas, till motsvarande före-ning med formeln (IV),definierad i patentkrav 3.
6. Förf arande enligt patentkrav 1, känneteck-5 n at av att nämnda med formeln (I) erhällna förening är en förening, väri R2 är 2-metoxifenyl och R3 är 3-klorfenyl, 3-trifluormetylfenyl eller fenyl.
7. Förf arande enligt patentkrav 1, känneteck-nat av att nämnda med formeln (I) erhällna förening är en 10 förening, väri R2 är 2-metoxifenyl och R3 är 3-klorfenyl.
8. Förf arande enligt patentkrav 1, känneteck-nat av att nämnda med formeln (I) erhällna förening är nägon av följande föreningar: : trans-2-fenyl-N-[(2-metoxifenyl)metyl]-1-azabicyk- ·· 15 lo [2.2.2]oktan-3-amin; ·. cis-2 - f enyl-N- (f enylmetyl) -1-azabicyklo [2.2.2] ok- tan-3-amin; • 2-(1-naftyl)-N-[(2-metoxifenyl)metyl]-1-azabicyklo- ! .* [2.2.2] oktan-3-amin; * » * 20 2-(1-naftyl)-N-[(2-trifluormetylfenyl)metyl]-1-aza- bicyklo[2.2.2]oktan-3-amin; > « ·’ 2-(3-klorfenyl) -N- [ (2-metoxifenyl) metyl]-1-azabi- cyklo [2.2.2] oktan-3-amin; ·;·· trans-2- (3-trifluormetylfenyl) -N- [ (2-metoxifenyl) - 25 metyl]-1-azabicyklo [2.2.2] oktan-3-amin; 2-(3-metoxifenyl)-N-[(2-metoxifenyl)-1-azabicyklo- “ [2.2.2]oktan-3-amin; *: 2-(4-metoxifenyl) -N- [ (2-metoxifenyl) metyl]-1-azabi cyklo [2.2.2]oktan-3-amin; 113654 2 -(2-klorfenyl)-N-[(2-metoxifenyl)metyl]-1-azabi-cyklo[2.2.2]oktan-3-amin; 2-(2-metoxifenyl)-N-[(2-metoxifenyl)metyl]-1-azabi-cyklo[2.2.2]oktan-3-amin och 5 2-fenyl-N-[(3,4-dimetoxifenyl)metyl]metyl-1-azabi- cyklo[2.2.2]oktan-3-amin. 1 · * · ' ·
FI925443A 1990-06-01 1992-11-30 Förfarande för framställning av terapeutiskt användbara azabicyklo[2.2.2]oktan-3-aminer FI113654B (sv)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
US53252590A 1990-06-01 1990-06-01
US53252590 1990-06-01
US9102853 1991-04-25
PCT/US1991/002853 WO1991018899A1 (en) 1990-06-01 1991-04-25 3-amino-2-aryl quinuclidines, process for their preparation and pharmaceutical compositions containing them

Publications (3)

Publication Number Publication Date
FI925443A0 FI925443A0 (fi) 1992-11-30
FI925443A FI925443A (fi) 1992-11-30
FI113654B true FI113654B (sv) 2004-05-31

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US (1) US5451586A (sv)
EP (1) EP0532527B1 (sv)
JP (1) JPH072740B2 (sv)
KR (1) KR930700499A (sv)
AT (1) ATE113947T1 (sv)
AU (1) AU648317B2 (sv)
CA (1) CA2084193C (sv)
DE (1) DE69105131T2 (sv)
DK (1) DK0532527T3 (sv)
ES (1) ES2063507T3 (sv)
FI (1) FI113654B (sv)
HU (1) HUT62891A (sv)
IE (1) IE911856A1 (sv)
IL (1) IL98259A0 (sv)
NO (1) NO924612L (sv)
PT (1) PT97771A (sv)
WO (1) WO1991018899A1 (sv)
ZA (1) ZA914134B (sv)

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NO924612D0 (no) 1992-11-30
PT97771A (pt) 1992-03-31
IL98259A0 (en) 1992-06-21
AU7860291A (en) 1991-12-31
CA2084193A1 (en) 1991-12-02
US5451586A (en) 1995-09-19
KR930700499A (ko) 1993-03-15
JPH072740B2 (ja) 1995-01-18
ES2063507T3 (es) 1995-01-01
NO924612L (no) 1992-11-30
EP0532527A1 (en) 1993-03-24
DK0532527T3 (da) 1995-01-02
HUT62891A (en) 1993-06-28
AU648317B2 (en) 1994-04-21
CA2084193C (en) 1998-04-07
ATE113947T1 (de) 1994-11-15
IE911856A1 (en) 1991-12-04
WO1991018899A1 (en) 1991-12-12
DE69105131T2 (de) 1995-03-23
HU9203777D0 (en) 1993-03-29
FI925443A0 (fi) 1992-11-30
DE69105131D1 (de) 1994-12-15
JPH05506243A (ja) 1993-09-16
ZA914134B (en) 1993-01-27
FI925443A (fi) 1992-11-30
EP0532527B1 (en) 1994-11-09

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