WO2010071358A3 - Method of preparing ezetimibe and intermediates used therein - Google Patents

Method of preparing ezetimibe and intermediates used therein Download PDF

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Publication number
WO2010071358A3
WO2010071358A3 PCT/KR2009/007535 KR2009007535W WO2010071358A3 WO 2010071358 A3 WO2010071358 A3 WO 2010071358A3 KR 2009007535 W KR2009007535 W KR 2009007535W WO 2010071358 A3 WO2010071358 A3 WO 2010071358A3
Authority
WO
WIPO (PCT)
Prior art keywords
intermediates used
ezetimibe
preparing ezetimibe
preparing
preventing
Prior art date
Application number
PCT/KR2009/007535
Other languages
French (fr)
Other versions
WO2010071358A2 (en
Inventor
Gi Jeong Kim
Choong Hahn Kim
Ji Yeon Chang
Nam Du Kim
Young Kil Chang
Gwan Sun Lee
Original Assignee
Hanmi Pharm. Co., 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 Hanmi Pharm. Co., Ltd. filed Critical Hanmi Pharm. Co., Ltd.
Publication of WO2010071358A2 publication Critical patent/WO2010071358A2/en
Publication of WO2010071358A3 publication Critical patent/WO2010071358A3/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/06Heterocyclic 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
    • C07D205/08Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D205/00Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings

Abstract

Disclosed is a method for preparing ezetimibe which is effective for preventing or treating arteriosclerosis, and novel intermediates used therein. In accordance with the method which does not use expensive reagents, unwanted diastereoisomers can be easily removed by a step-by-step crystallization procedure, and the ezetimibe of formula 1 can be prepared in a high yield without the use of a hydrogenation procedure under a high pressure.
PCT/KR2009/007535 2008-12-17 2009-12-16 Method of preparing ezetimibe and intermediates used therein WO2010071358A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2008-0128457 2008-12-17
KR20080128457 2008-12-17

Publications (2)

Publication Number Publication Date
WO2010071358A2 WO2010071358A2 (en) 2010-06-24
WO2010071358A3 true WO2010071358A3 (en) 2010-09-10

Family

ID=42269242

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2009/007535 WO2010071358A2 (en) 2008-12-17 2009-12-16 Method of preparing ezetimibe and intermediates used therein

Country Status (4)

Country Link
KR (1) KR101156588B1 (en)
AR (1) AR074752A1 (en)
TW (1) TW201028374A (en)
WO (1) WO2010071358A2 (en)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
WO2012076030A1 (en) 2010-12-10 2012-06-14 Pharmathen S.A. Process for the preparation of intermediate compounds useful in the preparation of ezetimibe
CN103086938A (en) * 2011-10-28 2013-05-08 沈阳药科大学 Ezetimibe synthesis method
CN103204795B (en) * 2012-01-11 2016-12-14 重庆华邦胜凯制药有限公司 A kind of preparation method of chirality azetidinones
CN103373970A (en) * 2012-04-16 2013-10-30 重庆圣华曦药业股份有限公司 Synthetic method for Ezetimibe intermediate
CN106831522B (en) * 2015-12-03 2021-06-08 中国科学院上海有机化学研究所 Lactam compound and preparation method thereof
CN106967106B (en) * 2017-04-24 2018-08-10 上海华源医药科技发展有限公司 A kind of production method of Ezetimibe intermediate
KR102078158B1 (en) 2018-02-21 2020-02-17 강원대학교산학협력단 Process for preparing Ezetimibe and intermediate thereof
US11110444B2 (en) 2019-12-30 2021-09-07 Industrial Technology Research Institute Chiral catalyst and heterogeneous chiral catalyst comprising the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
WO2007072088A1 (en) * 2005-12-20 2007-06-28 Richter Gedeon Nyrt. Process for the production of ezetimibe and intermediates used in this proces

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2353981C (en) * 1998-12-07 2005-04-26 Schering Corporation Process for the synthesis of azetidinones
KR20070063592A (en) * 2005-09-08 2007-06-19 테바 파마슈티컬 인더스트리즈 리미티드 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 (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
WO2007072088A1 (en) * 2005-12-20 2007-06-28 Richter Gedeon Nyrt. Process for the production of ezetimibe and intermediates used in this proces

Also Published As

Publication number Publication date
WO2010071358A2 (en) 2010-06-24
KR101156588B1 (en) 2012-06-20
AR074752A1 (en) 2011-02-09
KR20100070305A (en) 2010-06-25
TW201028374A (en) 2010-08-01

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