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AR090910A1 - Proceso mejorado para preparar rivaroxaban utilizando intermediarios - Google Patents

Proceso mejorado para preparar rivaroxaban utilizando intermediarios

Info

Publication number
AR090910A1
AR090910A1 ARP130101486A AR090910A1 AR 090910 A1 AR090910 A1 AR 090910A1 AR P130101486 A ARP130101486 A AR P130101486A AR 090910 A1 AR090910 A1 AR 090910A1
Authority
AR
Argentina
Prior art keywords
formula
rivaroxaban
racemic mixture
stereochemically isomeric
isomeric form
Prior art date
Application number
Other languages
English (en)
Inventor
Mohan Rao Dodda
Venkat Reddy Buthukuri
Original Assignee
Symed Labs Ltd
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 Symed Labs Ltd filed Critical Symed Labs Ltd
Publication of AR090910A1 publication Critical patent/AR090910A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00—Drugs for disorders of the blood or the extracellular fluid
    • A61P7/02—Antithrombotic agents; Anticoagulants; Platelet aggregation inhibitors
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D333/00—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom
    • C07D333/02—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings
    • C07D333/04—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom
    • C07D333/26—Heterocyclic compounds containing five-membered rings having one sulfur atom as the only ring hetero atom not condensed with other rings not substituted on the ring sulphur atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D333/38—Carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

El proceso en un solo recipiente que es industrialmente ventajoso para la preparación de Rivaroxaban o una forma estereoquímicamente isomérica o una mezcla racémica de las mismas, con alto rendimiento y pureza, utilizando intermediarios. El rivaroxaban es útil como inhibidor de la forma activa de coagulación X (factor Xa). Reivindicación 1: Un proceso en un solo recipiente para preparar Rivaroxaban, 5-cloro-N-[[(5S)-2-oxo-3-[4-(3-oxomorfolin-4-il)fenil]oxazolidin-5-il]metil]tiofeno-2-carboxamida, de fórmula (1), o una forma estereoquímicamente isomérica o una mezcla racémica de las mismas, caracterizado porque comprende: a) hacer reaccionar ácido 5-clorotiofeno-2-carboxílico de fórmula (4) o una sal del mismo, con un agente sulfonilante de fórmula (5a) ó (5b) donde R es un grupo alquilo, cicloalquilo, haloalquilo, aralquilo, o arilo sustituido o no sustituido; para producir un compuesto éster de sulfonilo de fórmula (3), donde R es según se lo definió anteriormente; b) hacer reaccionar el compuesto éster de sulfonilo de fórmula (3) con la 4-[4-[(5S)-5-(aminometil)-2-oxo-1,3-oxazolidin-3-il]fenil]morfolina-3-ona de fórmula (2) o una forma estereoquímicamente isomérica o una mezcla racémica de las mismas, o una sal de adición ácida de las mismas, para producir el Rivaroxaban de fórmula (1) o una forma estereoquímicamente isomérica o una mezcla racémica de las mismas. Reivindicación 15: Un compuesto éster de sulfonilo de fórmula (3), caracterizado porque R es un grupo alquilo, cicloalquilo, haloalquilo, aralquilo, o arilo sustituido o no sustituido.
ARP130101486 2012-05-02 2013-05-02 Proceso mejorado para preparar rivaroxaban utilizando intermediarios AR090910A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/IN2012/000321 WO2013164833A1 (en) 2012-05-02 2012-05-02 Improved process for preparing rivaroxaban using novel intermediates

Publications (1)

Publication Number Publication Date
AR090910A1 true AR090910A1 (es) 2014-12-17

Family

ID=49514278

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP130101486 AR090910A1 (es) 2012-05-02 2013-05-02 Proceso mejorado para preparar rivaroxaban utilizando intermediarios

Country Status (11)

Country Link
US (1) US9376427B2 (es)
EP (1) EP2844654B1 (es)
CN (1) CN104487436B (es)
AR (1) AR090910A1 (es)
AU (1) AU2012378913B2 (es)
BR (1) BR112014027248B1 (es)
CA (1) CA2871339C (es)
CY (1) CY1124179T1 (es)
ES (1) ES2871811T3 (es)
IL (1) IL235420A (es)
WO (1) WO2013164833A1 (es)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
IN2015DN02600A (es) * 2012-09-26 2015-09-18 Ranbaxy Lab Ltd
CN103558326B (zh) * 2013-11-12 2014-10-15 江苏正大清江制药有限公司 高效液相色谱法测定利伐沙班片中利伐沙班含量的方法
WO2015104605A1 (en) 2014-01-08 2015-07-16 Wockhardt Limited A process for preparing rivaroxaban or a pharmaceutically acceptable salt thereof
WO2015111076A2 (en) * 2014-01-23 2015-07-30 Symed Labs Limited Improved processes for the preparation of highly pure rivaroxaban crystal modification i
CN107778303B (zh) * 2016-08-27 2020-03-24 鲁南制药集团股份有限公司 利伐沙班的精制方法
SI3565552T1 (sl) 2017-01-04 2022-10-28 Unichem Laboratories Ltd Izboljšan postopek za pripravo rivaroksabana, ki vključuje nov intermediat

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DE19962924A1 (de) * 1999-12-24 2001-07-05 Bayer Ag Substituierte Oxazolidinone und ihre Verwendung
DE10300111A1 (de) * 2003-01-07 2004-07-15 Bayer Healthcare Ag Verfahren zur Herstellung von 5-Chlor-N-({(5S)-2-oxo-3-[4-(3-oxo-4-morpholinyl)-phenyl]-1,3-oxazolidin-5-yl}-methyl)-2-thiophencarboxamid
DE102004002044A1 (de) 2004-01-15 2005-08-04 Bayer Healthcare Ag Herstellverfahren
DE102007028406A1 (de) 2007-06-20 2008-12-24 Bayer Healthcare Ag Substituierte Oxazolidinone und ihre Verwendung
US7985750B2 (en) * 2007-08-14 2011-07-26 Concert Pharmaceuticals, Inc. Substituted oxazolidinone derivatives
US8309547B2 (en) * 2009-04-28 2012-11-13 Apotex Pharmachem Inc. Processes for the preparation of rivaroxaban and intermediates thereof
US7816355B1 (en) 2009-04-28 2010-10-19 Apotex Pharmachem Inc Processes for the preparation of rivaroxaban and intermediates thereof
EA031064B2 (ru) 2009-07-31 2020-07-01 КРКА, д.д., НОВО МЕСТО Способы кристаллизации ривароксабана
CN102822167A (zh) 2010-01-04 2012-12-12 埃南蒂亚有限公司 用于制备利伐沙班的方法及其中间体
EP2354128A1 (en) 2010-02-10 2011-08-10 Sandoz Ag Method for the preparation of rivaroxaban
EP2388260A1 (de) * 2010-05-21 2011-11-23 Archimica GmbH Herstellungsverfahren für einen Inhibitor eines Blutgerinnungsfaktors
WO2012156983A1 (en) * 2011-05-16 2012-11-22 Symed Labs Limited Processes for the preparation of 5-chloro-n-({(5s)-2-oxo-3-[4-(3-oxo-4-morpholinyl) phenyl]-1,3-oxazolidin-5-yl}methyl)-2-thiophenecarboxamide
CN102250077B (zh) * 2011-06-15 2013-11-13 浙江工业大学 一种利伐沙班中间体及其用于合成利伐沙班的方法

Also Published As

Publication number Publication date
EP2844654A4 (en) 2017-12-06
ES2871811T3 (es) 2021-11-02
US9376427B2 (en) 2016-06-28
AU2012378913A1 (en) 2014-11-13
BR112014027248B1 (pt) 2021-01-26
EP2844654B1 (en) 2021-03-10
CN104487436B (zh) 2017-05-24
EP2844654A1 (en) 2015-03-11
BR112014027248A2 (pt) 2017-06-27
AU2012378913B2 (en) 2017-04-13
CA2871339C (en) 2016-08-23
IL235420A (en) 2017-02-28
US20150126733A1 (en) 2015-05-07
CN104487436A (zh) 2015-04-01
WO2013164833A1 (en) 2013-11-07
CA2871339A1 (en) 2013-11-07
CY1124179T1 (el) 2022-05-27

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