HUP0400332A2 - Ipari eljárás tropenol előállítására - Google Patents

Ipari eljárás tropenol előállítására

Info

Publication number
HUP0400332A2
HUP0400332A2 HU0400332A HUP0400332A HUP0400332A2 HU P0400332 A2 HUP0400332 A2 HU P0400332A2 HU 0400332 A HU0400332 A HU 0400332A HU P0400332 A HUP0400332 A HU P0400332A HU P0400332 A2 HUP0400332 A2 HU P0400332A2
Authority
HU
Hungary
Prior art keywords
tropenol
formula
synthesis method
technical synthesis
produced
Prior art date
Application number
HU0400332A
Other languages
English (en)
Inventor
Armin Walter Rapp
Rainer Sobotta
Original Assignee
Boehringer Ingelheim Pharma Gmbh & Co. Kg
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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=7689774&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HUP0400332(A2) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Boehringer Ingelheim Pharma Gmbh & Co. Kg filed Critical Boehringer Ingelheim Pharma Gmbh & Co. Kg
Publication of HUP0400332A2 publication Critical patent/HUP0400332A2/hu
Publication of HUP0400332A3 publication Critical patent/HUP0400332A3/hu
Publication of HU230036B1 publication Critical patent/HU230036B1/hu

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P11/00Drugs for disorders of the respiratory system
    • A61P11/08Bronchodilators
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/04Centrally acting analgesics, e.g. opioids
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D451/00Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof
    • C07D451/02Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof
    • C07D451/04Heterocyclic compounds containing 8-azabicyclo [3.2.1] octane, 9-azabicyclo [3.3.1] nonane, or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane or granatane alkaloids, scopolamine; Cyclic acetals thereof containing not further condensed 8-azabicyclo [3.2.1] octane or 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring systems, e.g. tropane; Cyclic acetals thereof with hetero atoms directly attached in position 3 of the 8-azabicyclo [3.2.1] octane or in position 7 of the 3-oxa-9-azatricyclo [3.3.1.0<2,4>] nonane ring system
    • C07D451/06Oxygen atoms
    • C07D451/10Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (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)
  • Pulmonology (AREA)
  • Pain & Pain Management (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Lock And Its Accessories (AREA)
  • Catalysts (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)

Abstract

A találmány szerinti eljárással tropenolt oly módon állítják elő, hogyképletű tropenol tropenolt egy általános képletű szkopin-észterből -ahol R adott esetben szubsztituált alkil- vagy fenil-alkil-csoport -,előnyösen a képletű szkopolaminból vízben, aktiváló fémsókjelenlétében cinkkel végzett redukcióval, majd az intermedier bázissegítségével végzett hidrolízisével állítják elő, és adott esetbensójává a1akítják. A találmány tárgya továbbá a (II) képletű vegyületalkalmazása. Ó
HU0400332A 2001-06-28 2002-06-08 Ipari szintézis-eljárás tropenol előállítására HU230036B1 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE10131200 2001-06-28
DE10131200.8 2001-06-28
PCT/EP2002/006290 WO2003002562A1 (de) 2001-06-28 2002-06-08 Technische syntheseverfahren zur herstellung von tropenol

Publications (3)

Publication Number Publication Date
HUP0400332A2 true HUP0400332A2 (hu) 2004-08-30
HUP0400332A3 HUP0400332A3 (en) 2007-06-28
HU230036B1 HU230036B1 (hu) 2015-05-28

Family

ID=7689774

Family Applications (2)

Application Number Title Priority Date Filing Date
HU1400554A HU230379B1 (hu) 2001-06-28 2002-06-08 Tiotropium-bromid ipari előállítása
HU0400332A HU230036B1 (hu) 2001-06-28 2002-06-08 Ipari szintézis-eljárás tropenol előállítására

Family Applications Before (1)

Application Number Title Priority Date Filing Date
HU1400554A HU230379B1 (hu) 2001-06-28 2002-06-08 Tiotropium-bromid ipari előállítása

Country Status (41)

Country Link
US (1) US6610849B2 (hu)
EP (3) EP1404673B1 (hu)
JP (2) JP4485192B2 (hu)
KR (3) KR100866272B1 (hu)
CN (2) CN1982309B (hu)
AR (1) AR039056A1 (hu)
AT (3) ATE527257T1 (hu)
AU (2) AU2002257820B2 (hu)
BG (2) BG66398B1 (hu)
BR (1) BR0210664B1 (hu)
CA (1) CA2451573C (hu)
CO (1) CO5650166A2 (hu)
CY (1) CY1107681T1 (hu)
CZ (1) CZ296187B6 (hu)
DE (2) DE50209948D1 (hu)
DK (3) DK1404673T3 (hu)
EA (2) EA009808B1 (hu)
EC (1) ECSP034927A (hu)
EE (1) EE05403B1 (hu)
EG (1) EG23203A (hu)
ES (3) ES2242022T3 (hu)
HK (2) HK1068613A1 (hu)
HR (2) HRP20031085B1 (hu)
HU (2) HU230379B1 (hu)
IL (2) IL159239A0 (hu)
ME (1) MEP42608A (hu)
MX (1) MXPA03011516A (hu)
MY (1) MY122932A (hu)
NO (1) NO328154B1 (hu)
NZ (2) NZ530770A (hu)
PE (1) PE20030123A1 (hu)
PL (1) PL209520B1 (hu)
PT (2) PT1475379E (hu)
RS (1) RS50436B (hu)
SA (1) SA02230194B1 (hu)
SI (2) SI1475379T1 (hu)
SK (1) SK288022B6 (hu)
TW (1) TW574220B (hu)
UA (2) UA76761C2 (hu)
WO (1) WO2003002562A1 (hu)
ZA (1) ZA200308895B (hu)

Families Citing this family (12)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE10141377A1 (de) 2001-08-23 2003-03-13 Boehringer Ingelheim Pharma Aufstreuverfahren zur Herstellung von Pulverformulierungen
US6747153B2 (en) * 2002-05-31 2004-06-08 Boehringer Ingelheim Pharma Gmbh & Co. Kg Industrial process for preparing tropenol
US20090162562A1 (en) * 2007-12-24 2009-06-25 Bangalore Aswatha Nagaraj Methods for Applying Thermal Barrier Coating Systems
SI2240477T1 (sl) * 2008-01-10 2015-02-27 Generics (Uk) Limited Nov postopek za pripravo estrov skopina
CA2931876A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Anhydrate of tiotropium bromide
WO2011015884A1 (en) 2009-08-07 2011-02-10 Generics [Uk] Limited Process to prepare scopine esters
CN102351856B (zh) * 2011-08-24 2013-05-01 商丘市韶华药业有限公司 一种α-托品醇的纯化方法
ITRM20110508A1 (it) 2011-09-27 2013-03-28 Lusochimica Spa Processo per la preparazione degli esteri della scopina.
EP2607351B1 (en) * 2011-12-22 2017-03-15 Cerbios-Pharma S.A. Continuous process for the alkylation of cyclic tertiary amines
CN113292574B (zh) * 2020-02-21 2022-05-03 四川大学 一类手性多环的托品烷化合物及其制备方法和用途
CN111269226B (zh) * 2020-04-13 2021-09-21 石家庄四药有限公司 异丙托溴铵的合成方法
CN113264929B (zh) * 2021-05-02 2023-10-10 润生药业有限公司 一种噻托溴铵的制备方法

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE3931041C2 (de) * 1989-09-16 2000-04-06 Boehringer Ingelheim Kg Ester von Thienylcarbonsäuren mit Aminoalkoholen, ihre Quaternierungsprodukte, Verfahren zu ihrer Herstellung und diese enthaltende Arzneimittel
EP0756596B1 (en) * 1994-04-19 2002-08-21 Neurosearch A/S Tropane-2-aldoxime derivatives as neurotransmitter reuptake inhibitors
DE19515625C2 (de) * 1995-04-28 1998-02-19 Boehringer Ingelheim Kg Verfahren zur Herstellung von enantiomerenreinen Tropasäureestern

Also Published As

Publication number Publication date
HK1068613A1 (en) 2005-04-29
ZA200308895B (en) 2004-06-09
JP2004536830A (ja) 2004-12-09
BG111461A (en) 2013-08-30
EA200501081A1 (ru) 2006-06-30
TW574220B (en) 2004-02-01
SK288022B6 (sk) 2012-12-03
UA76761C2 (uk) 2006-09-15
NO20035633D0 (no) 2003-12-17
DK1475379T3 (da) 2007-09-03
IL159239A0 (en) 2004-06-01
MXPA03011516A (es) 2004-03-18
CO5650166A2 (es) 2006-06-30
YU101103A (en) 2006-05-25
ATE527257T1 (de) 2011-10-15
ECSP034927A (es) 2004-02-26
EP1475379B1 (de) 2007-04-11
NZ530770A (en) 2005-11-25
EP1475379A1 (de) 2004-11-10
HRP20031085A2 (en) 2004-04-30
PE20030123A1 (es) 2003-03-31
EA200301292A1 (ru) 2004-06-24
EE200400045A (et) 2004-04-15
PT1404673E (pt) 2005-07-29
HU230379B1 (hu) 2016-03-29
KR20030078793A (ko) 2003-10-08
PL209520B1 (pl) 2011-09-30
HUP0400332A3 (en) 2007-06-28
KR100886342B1 (ko) 2009-03-03
PL366942A1 (en) 2005-02-07
KR20080065313A (ko) 2008-07-11
DE50209948D1 (de) 2007-05-24
ES2285318T3 (es) 2007-11-16
HU230036B1 (hu) 2015-05-28
CN1982309B (zh) 2010-06-09
AU2008201565A1 (en) 2008-05-01
CN1288154C (zh) 2006-12-06
SI1404673T1 (en) 2005-10-31
RS50436B (sr) 2009-12-31
BG66398B1 (bg) 2013-12-31
EP1808435B1 (de) 2011-10-05
MEP42608A (en) 2011-02-10
NZ541395A (en) 2007-03-30
ATE359285T1 (de) 2007-05-15
EA009808B1 (ru) 2008-04-28
AU2008201565B2 (en) 2012-03-01
SK662004A3 (en) 2004-06-08
KR100530661B1 (ko) 2005-11-22
PT1475379E (pt) 2007-05-31
MY122932A (en) 2006-05-31
DE50203015D1 (de) 2005-06-09
JP4485192B2 (ja) 2010-06-16
ES2374981T3 (es) 2012-02-23
SA02230194B1 (ar) 2008-03-08
US20030022917A1 (en) 2003-01-30
KR100866272B1 (ko) 2008-11-03
CN1520413A (zh) 2004-08-11
NO328154B1 (no) 2009-12-21
BG108462A (bg) 2005-01-31
EE05403B1 (et) 2011-04-15
CA2451573C (en) 2010-09-21
HRP20090110A2 (en) 2009-04-30
EG23203A (en) 2004-07-31
KR20040023631A (ko) 2004-03-18
JP2010043116A (ja) 2010-02-25
ATE294801T1 (de) 2005-05-15
EP1808435A1 (de) 2007-07-18
EP1404673B1 (de) 2005-05-04
UA86031C2 (ru) 2009-03-25
AU2002257820B2 (en) 2008-05-08
CN1982309A (zh) 2007-06-20
US6610849B2 (en) 2003-08-26
CZ2004149A3 (cs) 2004-05-12
AR039056A1 (es) 2005-02-09
IL159239A (en) 2010-05-17
HRP20031085B1 (en) 2011-12-31
WO2003002562A1 (de) 2003-01-09
EP1404673A1 (de) 2004-04-07
ES2242022T3 (es) 2005-11-01
EA006393B1 (ru) 2005-12-29
CZ296187B6 (cs) 2006-01-11
BR0210664B1 (pt) 2013-12-03
CA2451573A1 (en) 2003-01-09
HK1103404A1 (en) 2007-12-21
DK1404673T3 (da) 2005-06-13
DK1808435T3 (da) 2012-01-16
CY1107681T1 (el) 2013-04-18
BR0210664A (pt) 2004-08-10
SI1475379T1 (sl) 2007-08-31

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