DE69716426T2 - Enantioselektive synthese von azetidinonen auf der basis von 3-hydroxy-gamma-lacton - Google Patents

Enantioselektive synthese von azetidinonen auf der basis von 3-hydroxy-gamma-lacton

Info

Publication number
DE69716426T2
DE69716426T2 DE69716426T DE69716426T DE69716426T2 DE 69716426 T2 DE69716426 T2 DE 69716426T2 DE 69716426 T DE69716426 T DE 69716426T DE 69716426 T DE69716426 T DE 69716426T DE 69716426 T2 DE69716426 T2 DE 69716426T2
Authority
DE
Germany
Prior art keywords
azetidinones
enantioselective synthesis
gamma lactone
hydroxy gamma
hydroxy
Prior art date
Legal status (The legal status 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 status listed.)
Expired - Lifetime
Application number
DE69716426T
Other languages
English (en)
Other versions
DE69716426D1 (de
Inventor
Guang-Zhong Wu
Xing Chen
Yee-Shing Wong
P Schumacher
Martin Steinman
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Merck Sharp and Dohme Corp
Original Assignee
Schering Corp
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 Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of DE69716426D1 publication Critical patent/DE69716426D1/de
Publication of DE69716426T2 publication Critical patent/DE69716426T2/de
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
DE69716426T 1996-05-31 1997-05-28 Enantioselektive synthese von azetidinonen auf der basis von 3-hydroxy-gamma-lacton Expired - Lifetime DE69716426T2 (de)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US08/655,785 US5739321A (en) 1996-05-31 1996-05-31 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones
PCT/US1997/009666 WO1997045406A1 (en) 1996-05-31 1997-05-28 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones

Publications (2)

Publication Number Publication Date
DE69716426D1 DE69716426D1 (de) 2002-11-21
DE69716426T2 true DE69716426T2 (de) 2003-08-14

Family

ID=24630339

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69716426T Expired - Lifetime DE69716426T2 (de) 1996-05-31 1997-05-28 Enantioselektive synthese von azetidinonen auf der basis von 3-hydroxy-gamma-lacton

Country Status (14)

Country Link
US (1) US5739321A (de)
EP (1) EP0906278B1 (de)
JP (1) JP3155759B2 (de)
AR (1) AR007314A1 (de)
AT (1) ATE226191T1 (de)
AU (1) AU3299497A (de)
CA (1) CA2255662C (de)
CO (1) CO4770966A1 (de)
DE (1) DE69716426T2 (de)
DK (1) DK0906278T3 (de)
ES (1) ES2185026T3 (de)
PT (1) PT906278E (de)
WO (1) WO1997045406A1 (de)
ZA (1) ZA974678B (de)

Families Citing this family (67)

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US5631365A (en) 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
WO2000034240A1 (en) * 1998-12-07 2000-06-15 Schering Corporation Process for the synthesis of azetidinones
US6207822B1 (en) 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
IL156550A0 (en) 2000-12-21 2004-01-04 Aventis Pharma Gmbh Novel 1,2-diphenzylazetidinones, method for producing the same, medicaments containing said compounds, and the use thereof for treating disorders of the lipid metabolism
US20060287254A1 (en) * 2001-01-26 2006-12-21 Schering Corporation Use of substituted azetidinone compounds for the treatment of sitosterolemia
PT1413331E (pt) * 2001-01-26 2007-12-18 Schering Corp Combinações do activador do receptor activado por proliferador do peroxisoma (ppar) fenofibrato e inibidor da absorção de esterol para indicações vasculares.
DE60206365T2 (de) 2001-03-28 2006-07-06 Schering Corporation, Kenilworth Verfahren für die enantioselektive synthese von azetidinon-zwischenprodukten
ATE345793T1 (de) * 2001-09-21 2006-12-15 Schering Corp Behandlung von xanthom mittels azetidinon- derivate als hemmer der sterol absorption
US20030204096A1 (en) * 2002-03-25 2003-10-30 Schering Corporation Enantioselective synthesis of azetidinone intermediate compounds
US7671047B2 (en) 2002-06-19 2010-03-02 Sanofi-Aventis Deutschland Gmbh Cationically substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
US7176194B2 (en) 2002-06-19 2007-02-13 Sanofi-Aventis Deutschland Gmbh Ring-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
US7176193B2 (en) 2002-06-19 2007-02-13 Sanofi-Aventis Deutschland Gmbh Acid-group-substituted diphenylazetidinones, process for their preparation, medicaments comprising these compounds, and their use
GB0215579D0 (en) * 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
US7135556B2 (en) * 2002-07-19 2006-11-14 Schering Corporation NPC1L1 (NPC3) and methods of use thereof
US7208486B2 (en) * 2003-03-07 2007-04-24 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
US7459442B2 (en) * 2003-03-07 2008-12-02 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
US7235543B2 (en) * 2003-03-07 2007-06-26 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
AR041089A1 (es) 2003-05-15 2005-05-04 Merck & Co Inc Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas
WO2005009955A1 (en) * 2003-07-31 2005-02-03 Hetero Drugs Limited Ezetimibe polymorphs
US7067675B2 (en) 2003-11-24 2006-06-27 Hetero Drugs Limited Process for ezetimibe intermediate
GB0329778D0 (en) * 2003-12-23 2004-01-28 Astrazeneca Ab Chemical compounds
ATE485267T1 (de) * 2003-12-23 2010-11-15 Astrazeneca Ab Diphenylazetidinonderivate mit die cholesterinabsorption hemmender wirkung
EP1723414A4 (de) * 2004-01-16 2008-03-26 Merck & Co Inc Npc1l1 (npc3) und verfahren zur identifizierung seiner liganden
US20060211752A1 (en) 2004-03-16 2006-09-21 Kohn Leonard D Use of phenylmethimazoles, methimazole derivatives, and tautomeric cyclic thiones for the treatment of autoimmune/inflammatory diseases associated with toll-like receptor overexpression
US20070244107A1 (en) * 2004-08-25 2007-10-18 Waters M Gerard Method of Treating Atherosclerosis, Dyslipidemias and Related Conditions
EP1817280A1 (de) * 2004-12-03 2007-08-15 Teva Pharmaceutical Industries Ltd. Ezetimib-polymorphe
US20060234996A1 (en) * 2005-04-14 2006-10-19 Itai Adin Novel crystalline form of ezetimibe and processes for the preparation thereof
KR20080021082A (ko) * 2005-06-20 2008-03-06 쉐링 코포레이션 히스타민 ｈ3 길항제로서 유용한 피페리딘 유도체
SA06270191B1 (ar) * 2005-06-22 2010-03-29 استرازينيكا ايه بي مشتقات من 2- أزيتيدينون جديدة باعتبارها مثبطات لامتصاص الكوليسترول لعلاج حالات فرط نسبة الدهون في الدم
AR054482A1 (es) * 2005-06-22 2007-06-27 Astrazeneca Ab Derivados de azetidinona para el tratamiento de hiperlipidemias
US20070049748A1 (en) * 2005-08-26 2007-03-01 Uppala Venkata Bhaskara R Preparation of ezetimibe
US20070259845A1 (en) * 2005-09-08 2007-11-08 Kansal Vinod K 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
US20080255084A1 (en) 2005-10-21 2008-10-16 Randy Lee Webb Combination of Organic Compounds
HU0501164D0 (en) * 2005-12-20 2006-02-28 Richter Gedeon Vegyeszet New industrial process for the production of ezetimibe
US20090227786A1 (en) * 2005-12-22 2009-09-10 Ana Gavalda I Escude Processes for preparing intermediate compounds useful for the preparation of ezetimibe
US7910698B2 (en) 2006-02-24 2011-03-22 Schering Corporation NPC1L1 orthologues
WO2007108007A1 (en) * 2006-03-23 2007-09-27 Unichem Laboratories Limited A process for the preparation of ezetimibe via a novel intermediate
AR060216A1 (es) * 2006-03-29 2008-06-04 Medichem Sa Procesos para preparar ezetimibe y compuestos intermediarios utiles para su preparacion
TW200811098A (en) * 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
BRPI0706041A2 (pt) * 2006-08-29 2011-03-22 Teva Pharmaceutichal Ind Ltd processos para purificação de (3r,4s)-4-(fenil-4-hydroxi-protegido)-1-(4-fluorofenil)- 3-[3-(4-fluorofenil)-3-oxoprofil]azetidina-2-ona
CA2661404A1 (en) * 2006-09-05 2008-03-13 Schering Corporation Pharmaceutical combinations for lipid management and in the treatment of atherosclerosis and hepatic steatosis
WO2008032338A2 (en) * 2006-09-11 2008-03-20 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe and its intermediates
JP2010509216A (ja) * 2006-11-02 2010-03-25 メルク エンド カムパニー インコーポレーテッド ヘテロシクリル置換抗高コレステロール血症化合物
US20090047716A1 (en) * 2007-06-07 2009-02-19 Nurit Perlman Reduction processes for the preparation of ezetimibe
US20080319221A1 (en) 2007-06-22 2008-12-25 Bernd Junker Esters of Pentahydroxyhexylcarbamoyl Alkanoic Acids
DE102007063671A1 (de) 2007-11-13 2009-06-25 Sanofi-Aventis Deutschland Gmbh Neue kristalline Diphenylazetidinonhydrate, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
CZ305066B6 (cs) * 2008-02-25 2015-04-22 Zentiva, K.S. Způsob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu
EP2128133A1 (de) * 2008-05-26 2009-12-02 Lek Pharmaceuticals D.D. Ezetiminverfahren und -zusammensetzung
PL387331A1 (pl) * 2009-02-24 2010-08-30 Instytut Chemii Organicznej Polskiej Akademii Nauk Sposób wytwarzania aldehydowego związku beta-laktamowego, związek pośredni, sposób wytwarzania związku pośredniego oraz zastosowanie związku pośredniego
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
EP2566497B1 (de) 2010-05-04 2015-07-29 Codexis, Inc. Biokatalysatoren zur ezetimib-synthese
ES2372460B1 (es) 2010-07-09 2012-11-16 Moehs Ibérica S.L. Nuevo método para la preparación de ezetimiba.
CN102477008B (zh) * 2010-11-22 2014-05-21 沈阳药科大学 依泽替米贝的合成方法
WO2012076030A1 (en) * 2010-12-10 2012-06-14 Pharmathen S.A. Process for the preparation of intermediate compounds useful in the preparation of ezetimibe
WO2012155932A1 (en) 2011-05-17 2012-11-22 Pharmathen S.A. Improved process for the preparation of ezetimibe
PL231215B1 (pl) 2011-06-15 2019-02-28 Inst Chemii Organicznej Polskiej Akademii Nauk Sposób wytwarzania podstawionych azetydynonów oraz związków pośrednich do ich syntezy
CN103086938A (zh) * 2011-10-28 2013-05-08 沈阳药科大学 依泽替米贝的合成方法
CN102531986A (zh) * 2012-02-23 2012-07-04 苏州朗科生物技术有限公司 一种依替米贝的制备方法
CN103570574B (zh) 2012-07-20 2016-04-13 中国科学院上海有机化学研究所 一种依泽替米贝的合成方法及该方法中所用的中间体
CN103044305A (zh) * 2013-01-24 2013-04-17 上海现代制药股份有限公司 一种依折麦布中间体的制备方法
WO2015039675A1 (en) 2013-09-23 2015-03-26 Pharmathen S.A. Novel process for the preparation of ezetimibe intermediates
CN103739537B (zh) * 2013-12-24 2015-05-20 连云港恒运医药科技有限公司 依折麦布的新合成方法
CN104072398B (zh) * 2014-07-03 2016-02-03 河南省科学院化学研究所有限公司 一种合成依折麦布的方法
JP2016145173A (ja) * 2015-02-09 2016-08-12 株式会社トクヤマ （３ｒ，４ｓ）‐１‐（４‐フルオロフェニル）‐［３（ｓ）‐ヒドロキシ‐３‐（４‐フルオロフェニル）プロピル］‐（４‐ヒドロキシフェニル）‐２‐アゼチジノンの製造方法
CN107098841A (zh) * 2016-02-19 2017-08-29 常州方楠医药技术有限公司 一种依折麦布的制备方法及该方法中所用的中间体
CN107033051A (zh) * 2017-06-08 2017-08-11 武汉励合生物医药科技有限公司 一种依泽替米贝的制备方法

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5631365A (en) * 1993-09-21 1997-05-20 Schering Corporation Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents
WO1997016424A1 (en) * 1995-11-02 1997-05-09 Schering Corporation Process for preparing 1-(4-fluorophenyl)-3(r)-(3(s)-hydroxy-3-([phenyl or 4-fluorophenyl])-propyl)-4(s)-(4-hydroxyphenyl)-2-azetidinone

Also Published As

Publication number Publication date
WO1997045406A1 (en) 1997-12-04
CA2255662A1 (en) 1997-12-04
ES2185026T3 (es) 2003-04-16
EP0906278A1 (de) 1999-04-07
ATE226191T1 (de) 2002-11-15
JP3155759B2 (ja) 2001-04-16
PT906278E (pt) 2003-01-31
EP0906278B1 (de) 2002-10-16
US5739321A (en) 1998-04-14
JPH11511754A (ja) 1999-10-12
CA2255662C (en) 2005-11-08
DK0906278T3 (da) 2003-02-17
DE69716426D1 (de) 2002-11-21
AU3299497A (en) 1998-01-05
CO4770966A1 (es) 1999-04-30
AR007314A1 (es) 1999-10-27
ZA974678B (en) 1997-11-28

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