WO2011024056A3 - An improved process for the preparation of bosentan - Google Patents

An improved process for the preparation of bosentan Download PDF

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Publication number
WO2011024056A3
WO2011024056A3 PCT/IB2010/002090 IB2010002090W WO2011024056A3 WO 2011024056 A3 WO2011024056 A3 WO 2011024056A3 IB 2010002090 W IB2010002090 W IB 2010002090W WO 2011024056 A3 WO2011024056 A3 WO 2011024056A3
Authority
WO
WIPO (PCT)
Prior art keywords
bosentan
preparation
improved process
deshydroxyethyl
sulfonamide
Prior art date
Application number
PCT/IB2010/002090
Other languages
French (fr)
Other versions
WO2011024056A2 (en
Inventor
Kumar Sinha Brajesh
Rajasekhara Raju Konduru
Shankar Reddy Budidet
Pandu Rangarao Vaddi
Islam Aminul
Sivakumaran Meenakshisunderam
Original Assignee
Aurobindo Pharma Limited
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 Aurobindo Pharma Limited filed Critical Aurobindo Pharma Limited
Publication of WO2011024056A2 publication Critical patent/WO2011024056A2/en
Publication of WO2011024056A3 publication Critical patent/WO2011024056A3/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
    • C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
    • C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
    • C07D239/46—Two or more oxygen, sulphur or nitrogen atoms
    • C07D239/52—Two oxygen atoms
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pulmonology (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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present application provides purification of Bosentan crude by making its crystalline potassium salt, which is further converted to Bosentan (I) with bis-sulfonamide (VIII) and deshydroxyethyl (IX) impurities to less than 0.2% by HPLC analysis.
PCT/IB2010/002090 2009-08-27 2010-08-27 An improved process for the preparation of bosentan WO2011024056A2 (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IN2065CH2009 2009-08-27
IN2065/CHE/2009 2009-08-27
IN2132/CHE/2010 2010-07-28
IN2132CH2010 2010-07-28

Publications (2)

Publication Number Publication Date
WO2011024056A2 WO2011024056A2 (en) 2011-03-03
WO2011024056A3 true WO2011024056A3 (en) 2011-05-19

Family

ID=43033160

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IB2010/002090 WO2011024056A2 (en) 2009-08-27 2010-08-27 An improved process for the preparation of bosentan

Country Status (1)

Country Link
WO (1) WO2011024056A2 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20130245259A1 (en) * 2012-03-16 2013-09-19 Natco Pharma Limited Process for the preparation of bosentan monohydrate
JP2015521594A (en) * 2012-06-12 2015-07-30 カディラ ファーマシューティカルズ リミテッド Method for producing bosentan
CN104193687B (en) * 2014-07-01 2017-09-26 上海天慈国际药业有限公司 A kind of preparation method for treating pulmonary hypertension medicine
BR112021005362A8 (en) 2018-10-03 2023-05-09 Huntsman Adv Mat Switzerland TRIAZINE UV ABSORBERS REPLACED WITH PYRIDINE AND PYRIMIDINE

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5292740A (en) * 1991-06-13 1994-03-08 Hoffmann-La Roche Inc. Sulfonamides
EP2072503A2 (en) * 2007-12-18 2009-06-24 Dipharma Francis S.r.l. Process for the preparation of bosentan
WO2009093127A2 (en) * 2008-01-24 2009-07-30 Actavis Group Ptc Ehf Substantially pure and a stable crystalline form of bosentan
WO2009095933A2 (en) * 2008-01-10 2009-08-06 Msn Laboratories Limited Improved and novel process for the preparation of bosentan
WO2010032261A1 (en) * 2008-08-12 2010-03-25 Cadila Healthcare Limited Process for preparation of bosentan
WO2010103362A2 (en) * 2009-03-11 2010-09-16 Sifavitor S.R.L. Process for the preparation of bosentan

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6136971A (en) 1998-07-17 2000-10-24 Roche Colorado Corporation Preparation of sulfonamides
EP2170841A1 (en) 2007-06-29 2010-04-07 Merck Generics (UK) Limited Process for introduction of hydroxyethoxy side chain in bosentan

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5292740A (en) * 1991-06-13 1994-03-08 Hoffmann-La Roche Inc. Sulfonamides
EP2072503A2 (en) * 2007-12-18 2009-06-24 Dipharma Francis S.r.l. Process for the preparation of bosentan
WO2009095933A2 (en) * 2008-01-10 2009-08-06 Msn Laboratories Limited Improved and novel process for the preparation of bosentan
WO2009093127A2 (en) * 2008-01-24 2009-07-30 Actavis Group Ptc Ehf Substantially pure and a stable crystalline form of bosentan
WO2010032261A1 (en) * 2008-08-12 2010-03-25 Cadila Healthcare Limited Process for preparation of bosentan
WO2010103362A2 (en) * 2009-03-11 2010-09-16 Sifavitor S.R.L. Process for the preparation of bosentan

Also Published As

Publication number Publication date
WO2011024056A2 (en) 2011-03-03

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