WO2008138605A3 - Verfahren zur herstellung von n-methylnaltrexonbromid - Google Patents

Verfahren zur herstellung von n-methylnaltrexonbromid Download PDF

Info

Publication number
WO2008138605A3
WO2008138605A3 PCT/EP2008/003870 EP2008003870W WO2008138605A3 WO 2008138605 A3 WO2008138605 A3 WO 2008138605A3 EP 2008003870 W EP2008003870 W EP 2008003870W WO 2008138605 A3 WO2008138605 A3 WO 2008138605A3
Authority
WO
WIPO (PCT)
Prior art keywords
bromide
producing
methylnaltrexone bromide
anion
leaving group
Prior art date
Application number
PCT/EP2008/003870
Other languages
English (en)
French (fr)
Other versions
WO2008138605A2 (de
Inventor
Ulrich Weigl
Pascal Schaer
Alfred Stutz
Original Assignee
Cilag Ag
Ulrich Weigl
Pascal Schaer
Alfred Stutz
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
Application filed by Cilag Ag, Ulrich Weigl, Pascal Schaer, Alfred Stutz filed Critical Cilag Ag
Priority to EP08758517.0A priority Critical patent/EP2167506B1/de
Priority to US12/600,341 priority patent/US8318936B2/en
Publication of WO2008138605A2 publication Critical patent/WO2008138605A2/de
Publication of WO2008138605A3 publication Critical patent/WO2008138605A3/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D489/00—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula:
    • C07D489/06—Heterocyclic compounds containing 4aH-8, 9 c- Iminoethano-phenanthro [4, 5-b, c, d] furan ring systems, e.g. derivatives of [4, 5-epoxy]-morphinan of the formula: with a hetero atom directly attached in position 14
    • C07D489/08—Oxygen atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/10—Laxatives
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Engineering & Computer Science (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)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Verfahren zur Herstellung von N-Methylnaltrexonbromid, wobei man eine Verbindung der allgemeinen Formel (I) : worin X' ein Anion, welches verschieden ist vom Bromidanion, und R Wasserstoff oder eine Abgangsgruppe, bedeuten, in einem geeigneten polaren Lösungsmittel löst oder dispergiert, diese Lösung oder Dispersion mit einer Verbindung, welche Bromidanionen enthält, mischt, und das erhaltene Reaktionsgemisch so lange rührt, bis das N-Methylnaltrexonbromid gebildet und kristallisiert ist, wobei man für den Fall, dass R eine Abgangsgruppe bedeutet, diese während oder nach der Umsetzung entfernt.
PCT/EP2008/003870 2007-05-16 2008-05-14 Verfahren zur herstellung von n-methylnaltrexonbromid WO2008138605A2 (de)

Priority Applications (2)

Application Number Priority Date Filing Date Title
EP08758517.0A EP2167506B1 (de) 2007-05-16 2008-05-14 Verfahren zur herstellung von n-methylnaltrexonbromid
US12/600,341 US8318936B2 (en) 2007-05-16 2008-05-14 Method for producing N-methylnaltrexone bromide

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
PCT/EP2007/004365 WO2008138383A1 (de) 2007-05-16 2007-05-16 Verfahren zur herstellung von n-methylnaltrexonbromid
EPPCT/EP07/004365 2007-05-16

Publications (2)

Publication Number Publication Date
WO2008138605A2 WO2008138605A2 (de) 2008-11-20
WO2008138605A3 true WO2008138605A3 (de) 2009-04-30

Family

ID=39156444

Family Applications (2)

Application Number Title Priority Date Filing Date
PCT/EP2007/004365 WO2008138383A1 (de) 2007-05-16 2007-05-16 Verfahren zur herstellung von n-methylnaltrexonbromid
PCT/EP2008/003870 WO2008138605A2 (de) 2007-05-16 2008-05-14 Verfahren zur herstellung von n-methylnaltrexonbromid

Family Applications Before (1)

Application Number Title Priority Date Filing Date
PCT/EP2007/004365 WO2008138383A1 (de) 2007-05-16 2007-05-16 Verfahren zur herstellung von n-methylnaltrexonbromid

Country Status (2)

Country Link
US (1) US8318936B2 (de)
WO (2) WO2008138383A1 (de)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
MX2011011245A (es) 2009-04-24 2012-04-11 Univ Brock Proceso para la preparacion de compuestos de morfinano.
US8580963B2 (en) 2010-11-05 2013-11-12 H. Lundbeck A/S Method for the manufacturing of naltrexone
JO3209B1 (ar) * 2010-11-05 2018-03-08 H Lundbeck As طريقة لتصنيع نالتريكسون
EA022266B1 (ru) * 2010-11-05 2015-11-30 Х. Лундбекк А/С Способ получения налтрексона
WO2013164383A1 (en) 2012-05-03 2013-11-07 H. Lundbeck A/S Method for the manufacturing of naltrexone
CN111777617A (zh) * 2020-07-10 2020-10-16 华润三九医药股份有限公司 一种溴甲纳曲酮的精制方法
EP4225312A1 (de) 2020-10-06 2023-08-16 Scilex Holding Company Orale verzögerte burst-formulierung von niedrigdosiertem naltrexon oder naloxon zur behandlung von fibromyalgie und langer covid

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004043964A2 (en) * 2002-11-08 2004-05-27 Mallinckrodt Inc. Process for the preparation of quaternary n-alkyl morphinan alkaloid salts
WO2006127899A2 (en) * 2005-05-25 2006-11-30 Progenics Pharmaceuticals, Inc. (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
WO2008034973A1 (fr) * 2006-09-21 2008-03-27 Sanofi-Aventis Procede de preparation d'halogenures de n-alkyl naltrexone

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004043964A2 (en) * 2002-11-08 2004-05-27 Mallinckrodt Inc. Process for the preparation of quaternary n-alkyl morphinan alkaloid salts
WO2006127899A2 (en) * 2005-05-25 2006-11-30 Progenics Pharmaceuticals, Inc. (r)-n-methylnaltrexone, processes for its synthesis and its pharmaceutical use
WO2008034973A1 (fr) * 2006-09-21 2008-03-27 Sanofi-Aventis Procede de preparation d'halogenures de n-alkyl naltrexone

Also Published As

Publication number Publication date
WO2008138383A1 (de) 2008-11-20
US20100168427A1 (en) 2010-07-01
US8318936B2 (en) 2012-11-27
WO2008138605A2 (de) 2008-11-20

Similar Documents

Publication Publication Date Title
WO2008138605A3 (de) Verfahren zur herstellung von n-methylnaltrexonbromid
WO2007003956A3 (en) Eutectic mixtures based upon multivalent metal ions
MX342850B (es) Proceso para la preparacion de triazolonas quirales.
MY157074A (en) Conversion method
JP2011506635A5 (de)
WO2010000506A3 (de) Verfahren zur herstellung freier carbonsäuren
WO2011109047A3 (en) Sulfomethylsuccinates, process for making same and compositions containing same
WO2007143454A3 (en) Process and apparatus for preparing a soap concentrate, a lubricating composition, and combinations thereof
EA200901175A1 (ru) Способ получения 2,6-дихлор-4-(трифторметил)фенилгидразина, используя смеси дихлор-фтор-трифторметилбензолов
SG144902A1 (en) Method and apparatus for obtaining purified phosphoric acid from phosphoric acid aqueous solution containing plural metal ions
WO2011091192A3 (en) Process for producing a copper thiometallate or a selenometallate material
ZA201002646B (en) Process for preparing 2-amino-5-cyanobenzoic acid derivatives
WO2008082502A3 (en) Process for preparing 2-amino-5-cyanobenzoic acid derivatives
UA102787C2 (ru) Способ приготовления кристаллических форм а и в илапразола и способ преобразования кристаллических форм
NZ592006A (en) Processes for the alkylation of secondary amine groups of morphinan derivatives
MY150973A (en) Method for producing diamine derivative
WO2010035190A3 (en) Method for producing phenolphthalein compound using ionic liquid catalyst composition
WO2007087434A3 (en) Method for the production of copper and zinc mono-and bi-metallic imidazolates
EP2495215A3 (de) Verfahren zur Herstellung von Monoperschwefelsäure und Vorrichtung zur kontinuierlichen Herstellung von Monoperschwefelsäure
WO2014024149A3 (en) Process for the colloidal synthesis of lithium iron phosphate
WO2009135598A8 (en) Process for preparing substituted biphenylanilides
ATE381571T1 (de) Verfahren zur herstellung von eisensaccharosekomplex
WO2013007582A3 (en) Processes for the preparation of thietanamine
WO2009066642A1 (ja) トリアゾール骨格を有する光応答性塩基
WO2009011421A1 (ja) 酸化剤とアミン系化合物の反応物を含有する解体性接着剤

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 08758517

Country of ref document: EP

Kind code of ref document: A2

NENP Non-entry into the national phase

Ref country code: DE

WWE Wipo information: entry into national phase

Ref document number: 2008758517

Country of ref document: EP

WWE Wipo information: entry into national phase

Ref document number: 12600341

Country of ref document: US