WO2010089764A3 - Improved process for preparation of nebivolol hydrochloride - Google Patents

Improved process for preparation of nebivolol hydrochloride Download PDF

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Publication number
WO2010089764A3
WO2010089764A3 PCT/IN2010/000004 IN2010000004W WO2010089764A3 WO 2010089764 A3 WO2010089764 A3 WO 2010089764A3 IN 2010000004 W IN2010000004 W IN 2010000004W WO 2010089764 A3 WO2010089764 A3 WO 2010089764A3
Authority
WO
WIPO (PCT)
Prior art keywords
benzopyran
dihydro
fluoro
nebivolol
preparation
Prior art date
Application number
PCT/IN2010/000004
Other languages
French (fr)
Other versions
WO2010089764A2 (en
Inventor
Manne Satyanarayana Reddy
Sajja Eswaraiah
Maramreddy Sahadeva Reddy
Original Assignee
Msn Laboratories 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 Msn Laboratories Limited filed Critical Msn Laboratories Limited
Publication of WO2010089764A2 publication Critical patent/WO2010089764A2/en
Publication of WO2010089764A3 publication Critical patent/WO2010089764A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D311/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings
    • C07D311/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only hetero atom, condensed with other rings ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D311/04—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring
    • C07D311/58—Benzo[b]pyrans, not hydrogenated in the carbocyclic ring other than with oxygen or sulphur atoms in position 2 or 4

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

An improved process for the preparation of nebivolol and its pharmaceutically acceptable salts is disclosed Concretely, the process involves a) esterifying 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylic acid to provide alkyl 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylate, b) reducing the alkyl 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxylate to provide 6-fluoro-3,4-dihydro-2H-l-benzopyran-2-carboxaldehyde, which is subsequently converted to 6-fluoro-3,4-dihydro-2-oxiranyl-2H-l-benzopyran, c) reacting 6-fluoro-3,4-dihydro-2-oxiranyl-2H-l-benzopyran with benzyl amine in a suitable solvent followed by treatment with suitable organic acid, and recrystalhzing the obtained compound to provide the corresponding organic acid salt of benzyl protected nebivolol, d) debenzylating the benzyl protected nebivolol salt, followed by treatment with hydrochloric acid to provide nebivolol hydrochloride
PCT/IN2010/000004 2009-01-05 2010-01-05 Improved process for the preparation of nebivolol hydrochloride WO2010089764A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN19CH2009 2009-01-05
IN19/CHE/2009 2009-01-05

Publications (2)

Publication Number Publication Date
WO2010089764A2 WO2010089764A2 (en) 2010-08-12
WO2010089764A3 true WO2010089764A3 (en) 2010-11-04

Family

ID=42542465

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2010/000004 WO2010089764A2 (en) 2009-01-05 2010-01-05 Improved process for the preparation of nebivolol hydrochloride

Country Status (1)

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WO (1) WO2010089764A2 (en)

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102329291A (en) * 2011-07-27 2012-01-25 上海现代制药股份有限公司 Method for preparing 6-fluoro-3,4-dihydro-2H-1-benzopyran-2-formaldehyde
ITRM20110418A1 (en) 2011-08-02 2013-02-03 Menarini Int Operations Lu Sa PROCESS FOR THE PREPARATION OF EPOXY WHICH INTERMEDIATES FOR THE SYNTHESIS OF NEBIVOLOL.
EP2907809B1 (en) 2014-02-14 2018-08-22 Corden Pharma International GmbH Base-free process for the preparation of ketone intermediates usable for manufacture of nebivolol
EP2907810A1 (en) 2014-02-14 2015-08-19 Corden Pharma International GmbH A new method for producing nebivolol hydrochloride of high purity
DE102014107132A1 (en) 2014-05-20 2015-11-26 Corden Pharma International Gmbh Process for the preparation of epoxides which can be used in the preparation of nebivolol and its derivatives
WO2016185492A1 (en) * 2015-05-19 2016-11-24 Ipca Laboratories Limited Process for preparation of nebivolol and it's salts

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4654362A (en) * 1983-12-05 1987-03-31 Janssen Pharmaceutica, N.V. Derivatives of 2,2'-iminobisethanol
WO2004041805A1 (en) * 2002-11-06 2004-05-21 EGIS Gyógyszergyár Rt. NEW PROCESS FOR THE PREPARATION OF RACEMIC ([2S[2R*[R[R*]]]] and ([2R[2S*[S[S*]]]]-(±)- α,α' -[imino-bis(methylene)]bis[6-fluoro­chroman-2-methanol] AND ITS PURE [2S[2R*[R[R*]&
WO2006016376A1 (en) * 2004-08-11 2006-02-16 Hetero Drugs Limited A novel process for preparation of nebivolol intermediates
WO2006025070A2 (en) * 2004-07-30 2006-03-09 Torrent Pharmaceuticals Limited Nebivolol and its pharmaceutically acceptable salts, process for preparation and pharmaceutical compositions of nebivolol

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4654362A (en) * 1983-12-05 1987-03-31 Janssen Pharmaceutica, N.V. Derivatives of 2,2'-iminobisethanol
WO2004041805A1 (en) * 2002-11-06 2004-05-21 EGIS Gyógyszergyár Rt. NEW PROCESS FOR THE PREPARATION OF RACEMIC ([2S[2R*[R[R*]]]] and ([2R[2S*[S[S*]]]]-(±)- α,α' -[imino-bis(methylene)]bis[6-fluoro­chroman-2-methanol] AND ITS PURE [2S[2R*[R[R*]&
WO2006025070A2 (en) * 2004-07-30 2006-03-09 Torrent Pharmaceuticals Limited Nebivolol and its pharmaceutically acceptable salts, process for preparation and pharmaceutical compositions of nebivolol
WO2006016376A1 (en) * 2004-08-11 2006-02-16 Hetero Drugs Limited A novel process for preparation of nebivolol intermediates

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DATABASE CASREACT 6 November 2009 (2009-11-06), Database accession no. 152:525671 *

Also Published As

Publication number Publication date
WO2010089764A2 (en) 2010-08-12

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