WO2009157019A3 - Process for preparing ezetimibe using novel allyl intermediates - Google Patents

Process for preparing ezetimibe using novel allyl intermediates Download PDF

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Publication number
WO2009157019A3
WO2009157019A3 PCT/IN2009/000358 IN2009000358W WO2009157019A3 WO 2009157019 A3 WO2009157019 A3 WO 2009157019A3 IN 2009000358 W IN2009000358 W IN 2009000358W WO 2009157019 A3 WO2009157019 A3 WO 2009157019A3
Authority
WO
WIPO (PCT)
Prior art keywords
novel allyl
preparing ezetimibe
ezetimibe
intermediates
allyl intermediates
Prior art date
Application number
PCT/IN2009/000358
Other languages
French (fr)
Other versions
WO2009157019A2 (en
Inventor
Srinivasan Chidambaram Venkateswaran
Singh Sarin Gurdeep
Pranav Gupta
Lalit Wadhwa
Original Assignee
Ind-Swift 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 Ind-Swift Laboratories Limited filed Critical Ind-Swift Laboratories Limited
Publication of WO2009157019A2 publication Critical patent/WO2009157019A2/en
Publication of WO2009157019A3 publication Critical patent/WO2009157019A3/en

Links

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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/26—Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The present invention provides an efficient and industrially advantageous process for the preparation of ezetimibe of formula (I), using novel intermediates.
PCT/IN2009/000358 2008-06-23 2009-06-23 Process for preparing ezetimibe using novel allyl intermediates WO2009157019A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
IN1498/DEL/2008 2008-06-23
IN1498DE2008 2008-06-23

Publications (2)

Publication Number Publication Date
WO2009157019A2 WO2009157019A2 (en) 2009-12-30
WO2009157019A3 true WO2009157019A3 (en) 2010-09-30

Family

ID=41445058

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/IN2009/000358 WO2009157019A2 (en) 2008-06-23 2009-06-23 Process for preparing ezetimibe using novel allyl intermediates

Country Status (1)

Country Link
WO (1) WO2009157019A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103962180A (en) * 2013-08-06 2014-08-06 汕头大学 Salen coordination polymer catalyst for preparing alpha-aminonitrile and preparation method of catalyst

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2414529A2 (en) 2009-04-01 2012-02-08 Matrix Laboratories Ltd 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
CN102008978B (en) * 2010-11-24 2012-10-03 郑州大学 Chiral catalyst and preparation method and application thereof
CN102531985B (en) * 2011-04-25 2013-12-18 开原亨泰制药股份有限公司 Method for preparing ezetimibe key intermediate
CN103086938A (en) * 2011-10-28 2013-05-08 沈阳药科大学 Ezetimibe synthesis method
US20160362369A1 (en) * 2014-03-06 2016-12-15 Nissan Chemical Industries, Ltd. Method for producing optically active azetidinone compound
CN104072398B (en) * 2014-07-03 2016-02-03 河南省科学院化学研究所有限公司 A kind of method of synthesizing Ezetimibe
CN105717204B (en) * 2014-12-04 2018-03-02 天津药物研究院有限公司 A kind of detection method of Ezetimibe optical isomer and its application
CN107118144B (en) * 2016-02-24 2020-04-10 上海医药工业研究院 Reduction preparation process of ezetimibe and intermediate thereof
WO2017168438A1 (en) * 2016-03-31 2017-10-05 Ind-Swift Laboratories Limited Process for preparing pure allyl protected keto derivative
CN108976186B (en) * 2017-06-01 2021-12-10 中国科学院大连化学物理研究所 Method for preparing tetra-substituted furan compound based on carbon-hydrogen bond activation
CN112409212B (en) * 2020-11-30 2023-03-14 四川新迪医药化工有限公司 Preparation method of citalopram diol intermediate hydrobromide, citalopram diol intermediate hydrobromide and citalopram

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021497A2 (en) * 2003-08-28 2005-03-10 Microbia, Inc. Tethered dimers and trimers of 1,4-diphenylazetidn-2-ones
WO2006127893A2 (en) * 2005-05-25 2006-11-30 Microbia, Inc. Processes for production of 4-(biphenylyl)azetidin-2-one phosphonic acids
US20070049748A1 (en) * 2005-08-26 2007-03-01 Uppala Venkata Bhaskara R Preparation of ezetimibe
WO2008096372A2 (en) * 2007-02-06 2008-08-14 Ind-Swift Laboratories Limited Process for preparing highly pure ezetimibe using novel intermediates

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2005021497A2 (en) * 2003-08-28 2005-03-10 Microbia, Inc. Tethered dimers and trimers of 1,4-diphenylazetidn-2-ones
WO2006127893A2 (en) * 2005-05-25 2006-11-30 Microbia, Inc. Processes for production of 4-(biphenylyl)azetidin-2-one phosphonic acids
US20070049748A1 (en) * 2005-08-26 2007-03-01 Uppala Venkata Bhaskara R Preparation of ezetimibe
WO2008096372A2 (en) * 2007-02-06 2008-08-14 Ind-Swift Laboratories Limited Process for preparing highly pure ezetimibe using novel intermediates

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
GUIBE, F.: "Allylic Protecting Groups and Their Use in a Complex Environment. Part I : Allylic Protection of Alcohols.", TETRAHEDRON, vol. 53, no. 40, 1997, pages 13509 - 13556 *

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN103962180A (en) * 2013-08-06 2014-08-06 汕头大学 Salen coordination polymer catalyst for preparing alpha-aminonitrile and preparation method of catalyst
CN103962180B (en) * 2013-08-06 2016-02-17 汕头大学 For the preparation of the Salen coordination polymer Catalysts and its preparation method of alpha-aminonitriles

Also Published As

Publication number Publication date
WO2009157019A2 (en) 2009-12-30

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