WO2008032338A3 - Improved process for the preparation of ezetimibe and its intermediates - Google Patents

Improved process for the preparation of ezetimibe and its intermediates Download PDF

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Publication number
WO2008032338A3
WO2008032338A3 PCT/IN2007/000400 IN2007000400W WO2008032338A3 WO 2008032338 A3 WO2008032338 A3 WO 2008032338A3 IN 2007000400 W IN2007000400 W IN 2007000400W WO 2008032338 A3 WO2008032338 A3 WO 2008032338A3
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WO
WIPO (PCT)
Prior art keywords
ezetimibe
preparation
improved process
intermediates
present
Prior art date
Application number
PCT/IN2007/000400
Other languages
French (fr)
Other versions
WO2008032338A2 (en
Inventor
Manne Satyanarayana Reddy
Maramreddy Sahadeva Reddy
Original Assignee
Manne Satyanarayana Reddy
Maramreddy Sahadeva Reddy
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 Manne Satyanarayana Reddy, Maramreddy Sahadeva Reddy filed Critical Manne Satyanarayana Reddy
Publication of WO2008032338A2 publication Critical patent/WO2008032338A2/en
Publication of WO2008032338A3 publication Critical patent/WO2008032338A3/en

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Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D205/08—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with one oxygen atom directly attached in position 2, e.g. beta-lactams

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The present invention provides an improved process for the preparation of ezetimibe through novel organic amine salt compounds of general formula (1). The present invention also relates to a highly pure ezetimibe and 3-((3R,4S)-1-(4-fluorophenyl)-2-oxo-4-(4-(benzyloxy)phenyl) azetidin-3-yl)propionic acid compound.
PCT/IN2007/000400 2006-09-11 2007-09-10 Improved process for the preparation of ezetimibe and its intermediates WO2008032338A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1648/CHE/2006 2006-09-11
IN1648CH2006 2006-09-11

Publications (2)

Publication Number Publication Date
WO2008032338A2 WO2008032338A2 (en) 2008-03-20
WO2008032338A3 true WO2008032338A3 (en) 2009-10-15

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2007/000400 WO2008032338A2 (en) 2006-09-11 2007-09-10 Improved process for the preparation of ezetimibe and its intermediates

Country Status (1)

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WO (1) WO2008032338A2 (en)

Families Citing this family (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1893570A4 (en) * 2005-06-22 2009-12-23 Reddy Manne Satynarayana Improved process for the preparation of ezetimibe
EP2965752A1 (en) * 2007-12-10 2016-01-13 ratiopharm GmbH Pharmaceutical formulation comprising ezetimibe
EP2128133A1 (en) * 2008-05-26 2009-12-02 Lek Pharmaceuticals D.D. Ezetimibe process and composition
EP2149547A1 (en) * 2008-07-30 2010-02-03 LEK Pharmaceuticals D.D. Process for the synthesis of ezetimibe and intermediates useful therefor
US9388440B2 (en) 2009-04-01 2016-07-12 Mylan Laboratories Limited Enzymatic process for the preparation of (S)-5-(4-fluoro-phenyl)-5-hydroxy-1morpholin-4-yl-pentan-1-one, an intermediate of Ezetimibe and further conversion to Ezetimibe
CN102675177A (en) * 2011-06-28 2012-09-19 常州制药厂有限公司 Preparation methods of blood fat lowering medicament and key intermediates of blood fat lowering medicament
CN103755616A (en) * 2013-12-31 2014-04-30 北京万全德众医药生物技术有限公司 Method for preparing ezetimibe isomer
CN104387308A (en) * 2014-11-18 2015-03-04 武汉福星生物药业有限公司 Method for preparing high-purity ezetimibe by controlling generation of EZ-zanOH impurity
CN105566243B (en) * 2016-01-15 2017-10-31 齐鲁天和惠世制药有限公司 The method that the oxazolidone of (s) (+) 4 phenyl 2 is reclaimed from Ezetimibe production waste liquid
CN107129452A (en) * 2016-02-26 2017-09-05 常州制药厂有限公司 A kind of preparation method of blood lipid-lowering medicine ezetimibe and its key intermediate

Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1995001961A1 (en) * 1993-07-09 1995-01-19 Schering Corporation Process for the synthesis of azetidinones
US5561227A (en) * 1991-07-23 1996-10-01 Schering Corporation Process for the stereospecific synthesis of azetidinones
WO1997045406A1 (en) * 1996-05-31 1997-12-04 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
WO2005009955A1 (en) * 2003-07-31 2005-02-03 Hetero Drugs Limited Ezetimibe polymorphs
WO2006137080A1 (en) * 2005-06-22 2006-12-28 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe
WO2007030721A2 (en) * 2005-09-08 2007-03-15 Teva Pharmaceutical Industries Ltd. Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe

Patent Citations (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5561227A (en) * 1991-07-23 1996-10-01 Schering Corporation Process for the stereospecific synthesis of azetidinones
WO1995001961A1 (en) * 1993-07-09 1995-01-19 Schering Corporation Process for the synthesis of azetidinones
WO1997045406A1 (en) * 1996-05-31 1997-12-04 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
WO2005009955A1 (en) * 2003-07-31 2005-02-03 Hetero Drugs Limited Ezetimibe polymorphs
WO2006137080A1 (en) * 2005-06-22 2006-12-28 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe
WO2007030721A2 (en) * 2005-09-08 2007-03-15 Teva Pharmaceutical Industries Ltd. Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PROCESS CHEMISTRY IN THE PHARMACEUTICAL INDUSTRY, vol. 1, 1999, DEKKER, NEW YORK, pages 221 - 242 *

Also Published As

Publication number Publication date
WO2008032338A2 (en) 2008-03-20

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