AR057690A1 - Procedimiento para preparar sales de tiotropio - Google Patents

Procedimiento para preparar sales de tiotropio

Info

Publication number
AR057690A1
AR057690A1 ARP060103225A ARP060103225A AR057690A1 AR 057690 A1 AR057690 A1 AR 057690A1 AR P060103225 A ARP060103225 A AR P060103225A AR P060103225 A ARP060103225 A AR P060103225A AR 057690 A1 AR057690 A1 AR 057690A1
Authority
AR
Argentina
Prior art keywords
formula
compound
group
anion
kat
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.)
Pending
Application number
ARP060103225A
Other languages
English (en)
Inventor
Joerg Brandenburg
Waldemar Pfrengle
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.)
Boehringer Ingelheim Pharma GmbH Co KG
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
Application filed by Boehringer Ingelheim Pharma GmbH Co KG filed Critical Boehringer Ingelheim Pharma GmbH Co KG
Publication of AR057690A1 publication Critical patent/AR057690A1/es
Pending legal-status Critical Current

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • C07D451/06—Oxygen atoms
    • C07D451/10—Oxygen atoms acylated by aliphatic or araliphatic carboxylic acids, e.g. atropine, scopolamine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
    • 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
    • A61P11/00—Drugs for disorders of the respiratory system
    • A61P11/06—Antiasthmatics
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D451/00—Heterocyclic 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
    • C07D451/02—Heterocyclic 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
    • C07D451/04—Heterocyclic 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
    • C07D451/06—Oxygen atoms

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pulmonology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Emergency Medicine (AREA)
  • Epidemiology (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

La invencion se refiere a un nuevo procedimiento para preparar sales de tiotropio. Reivindicacion 1: Procedimiento para preparar sales de tiotropio de formula (1) en las cuales X - puede significar un anion con carga negativa sencilla, caracterizado porque se hace reaccionar un compuesto de formula (2) en el cual Y - puede significar un anion lipofilo con carga negativa sencilla, distinto de X -, con preferencia un anion seleccionado del grupo compuesto por hexafluorofosfato, tetrafluoroborato, tetrafenilborato y sacarinato, de manera especialmente preferida hexafluorofosfato o tetrafenilborato. en un solo paso, con un compuesto de formula (3) en el cual R significa un radical seleccionado del grupo compuesto por metoxi, etoxi, propoxi, isopropoxi, isopropeniloxi, butoxi, O-N-succinimida, O-N-fralimida, feniloxi, nitrofeniloxi, fluorofeniloxi, pentafluorofeniloxi, viniloxi, 2-aliloxi, -S-metilo, -S-etilo y -S-fenilo, en un disolvente adecuado, y con adicion de una base adecuada, para proporcionar un compuesto de formula (4) pudiendo tener el grupo Y- los significados antes indicados, y se transforma el compuesto de formula 4, sin aislarlo, mediante reaccion con una sal Kat+X-, representado Kat+ un cation seleccionado del grupo compuesto por Li+, Na+, K+, Mg2+, Ca2+ y cationes orgánicos con N cuaternario por ejemplo N,N-dialquil-imidazolio, tetra-alquilamonio) y X- puede tener los significados antes indicados, en el compuesto de formula 1.
ARP060103225A 2005-07-27 2006-07-26 Procedimiento para preparar sales de tiotropio Pending AR057690A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE102005035112A DE102005035112A1 (de) 2005-07-27 2005-07-27 Neues Verfahren zur Herstellung von Tiotropiumsalzen unter Anwendung von in organischen Lösungsmitteln löslichen N-Methylscopiniumsalzen

Publications (1)

Publication Number Publication Date
AR057690A1 true AR057690A1 (es) 2007-12-12

Family

ID=37110331

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP060103225A Pending AR057690A1 (es) 2005-07-27 2006-07-26 Procedimiento para preparar sales de tiotropio

Country Status (24)

Country Link
US (5) US20070027320A1 (es)
EP (2) EP1910354B1 (es)
JP (1) JP5210861B2 (es)
KR (1) KR101299929B1 (es)
CN (2) CN104356129A (es)
AR (1) AR057690A1 (es)
AU (1) AU2006274012B2 (es)
BR (1) BRPI0614062B8 (es)
CA (1) CA2616222C (es)
DE (1) DE102005035112A1 (es)
DK (1) DK1910354T3 (es)
EA (1) EA014271B1 (es)
EC (1) ECSP088138A (es)
ES (1) ES2613952T3 (es)
HU (1) HUE032259T2 (es)
IL (1) IL188989A (es)
MX (1) MX2008001093A (es)
NO (2) NO340877B1 (es)
NZ (1) NZ566039A (es)
PL (1) PL1910354T3 (es)
TW (3) TWI443097B (es)
UA (1) UA94914C2 (es)
WO (1) WO2007012626A2 (es)
ZA (1) ZA200711113B (es)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2008089852A1 (de) * 2007-01-26 2008-07-31 Boehringer Ingelheim Pharma Gmbh & Co.Kg Neues verfahren zur herstellung von tiotropiumsalzen
EP1950196A1 (de) * 2007-01-29 2008-07-30 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung von Ammoniumhexafluorophosphaten
EP1953156A1 (de) * 2007-01-29 2008-08-06 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung von Scopiniumsalzen
EP1997819A1 (de) * 2007-05-25 2008-12-03 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung von Scopinestern
EP2036898A2 (de) * 2007-09-13 2009-03-18 Boehringer Ingelheim Pharma GmbH & Co. KG Verfahren zur Herstellung von 1,3-Dioxolan-2Onen sowie von Carbonsäureestern durch Transacylierung unter Basischen Reaktionsbedingungen
US20110028508A1 (en) * 2008-01-10 2011-02-03 Gemerocs [UK] Limited Novel process for the preparation of scopine esters
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
CZ305012B6 (cs) * 2012-03-30 2015-03-25 Zentiva, K.S. Způsob přípravy skopinesteru kyseliny di(2-thienyl)glykolové, intermediátu v syntéze tiotropium bromidu
WO2021133280A1 (en) * 2019-12-27 2021-07-01 Deva Holding An improved process for preparation of scopine hydrobromide

Family Cites Families (18)

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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
US7441045B2 (en) * 1999-12-13 2008-10-21 F5 Networks, Inc. Method and system for balancing load distribution on a wide area network
US6934686B1 (en) 2000-06-30 2005-08-23 I2 Technologies Us, Inc. Warranty transaction system and method
US7574499B1 (en) * 2000-07-19 2009-08-11 Akamai Technologies, Inc. Global traffic management system using IP anycast routing and dynamic load-balancing
US6706726B2 (en) * 2000-10-14 2004-03-16 Boehringer Ingelheim Pharma Gmbh & Co. Kg Anticholinergics which may be used as medicaments as well as processes for preparing them
DE10064816A1 (de) * 2000-12-22 2002-06-27 Boehringer Ingelheim Pharma Verfahren zur Herstellung eines Anticholinergikums
US6506900B1 (en) * 2001-01-31 2003-01-14 Boehringer Ingelheim Pharma Ag Process for preparing a scopine ester intermediate
US7237017B1 (en) * 2001-03-13 2007-06-26 Panamsat Corporation Micronode in a satellite based content delivery system
US7340505B2 (en) * 2001-04-02 2008-03-04 Akamai Technologies, Inc. Content storage and replication in a managed internet content storage environment
DE60216588T2 (de) * 2001-05-25 2007-09-20 Boehringer Ingelheim Pharma Gmbh & Co. Kg Kombination eines pde4-inhibitors mit tiotropium zur behandlung obstruktiver atemwegserkrankungen
EP2403219B1 (en) * 2001-09-28 2014-10-22 Level 3 CDN International, Inc. Method for name to address resolution
DE10200943A1 (de) * 2002-01-12 2003-07-24 Boehringer Ingelheim Pharma Verfahren zur Herstellung von Scopinestern
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EP1504756A1 (en) * 2003-08-06 2005-02-09 Kyowa Hakko Kogyo Co., Ltd Medicament compositions comprising a heterocyclic compound and an anticholinergic
KR20060117334A (ko) * 2003-11-03 2006-11-16 베링거 인겔하임 인터내셔날 게엠베하 티오트로피움 염의 제조방법, 티오트로피움 염 및 이를함유하는 약제학적 조성물
CA2544357A1 (en) * 2003-11-03 2005-05-12 Boehringer Ingelheim International Gmbh Tiotropium salts, methods for the production thereof, and pharmaceutical formulations containing the same
DE102004041253A1 (de) * 2004-08-26 2006-03-02 Boehringer Ingelheim Pharma Gmbh & Co. Kg Neues Verfahren zur Herstellung von Tiotropiumsalzen
KR20080024532A (ko) * 2005-06-15 2008-03-18 베링거 인겔하임 인터내셔날 게엠베하 신규한 티오트로퓸 염의 제조방법, 신규한 티오트로퓸 염및 이의 약제학적 조성물

Also Published As

Publication number Publication date
MX2008001093A (es) 2008-03-11
TW201418252A (zh) 2014-05-16
TWI443097B (zh) 2014-07-01
AU2006274012A1 (en) 2007-02-01
BRPI0614062A2 (pt) 2011-03-09
NO20076681L (no) 2008-02-13
UA94914C2 (ru) 2011-06-25
BRPI0614062B1 (pt) 2020-11-17
DE102005035112A1 (de) 2007-02-15
EA014271B1 (ru) 2010-10-29
US20100210844A1 (en) 2010-08-19
CN101309920A (zh) 2008-11-19
US20070027320A1 (en) 2007-02-01
IL188989A (en) 2012-10-31
BRPI0614062B8 (pt) 2021-05-25
CN104356129A (zh) 2015-02-18
TWI486345B (zh) 2015-06-01
TWI486346B (zh) 2015-06-01
JP5210861B2 (ja) 2013-06-12
ECSP088138A (es) 2008-02-20
HUE032259T2 (en) 2017-09-28
EP1910354A2 (de) 2008-04-16
US20140323732A1 (en) 2014-10-30
KR101299929B1 (ko) 2013-08-27
NZ566039A (en) 2011-07-29
CA2616222A1 (en) 2007-02-01
EP1910354B1 (de) 2016-11-09
EP3153512A1 (de) 2017-04-12
TW200738704A (en) 2007-10-16
AU2006274012B2 (en) 2011-11-03
ES2613952T3 (es) 2017-05-29
KR20080032634A (ko) 2008-04-15
ZA200711113B (en) 2010-08-25
EA200800324A1 (ru) 2008-08-29
CA2616222C (en) 2014-09-23
TW201418253A (zh) 2014-05-16
NO340877B1 (no) 2017-07-03
IL188989A0 (en) 2008-08-07
US20150225395A1 (en) 2015-08-13
WO2007012626A3 (de) 2010-05-06
NO20170613A1 (no) 2008-02-13
JP2009507769A (ja) 2009-02-26
WO2007012626A2 (de) 2007-02-01
PL1910354T3 (pl) 2017-04-28
DK1910354T3 (en) 2017-02-13
US20130116435A1 (en) 2013-05-09

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