ZA974678B - 3-Hydroxy gamma-lactone based enantioselective synthesis of azetidinones. - Google Patents

3-Hydroxy gamma-lactone based enantioselective synthesis of azetidinones.

Info

Publication number
ZA974678B
ZA974678B ZA9704678A ZA974678A ZA974678B ZA 974678 B ZA974678 B ZA 974678B ZA 9704678 A ZA9704678 A ZA 9704678A ZA 974678 A ZA974678 A ZA 974678A ZA 974678 B ZA974678 B ZA 974678B
Authority
ZA
South Africa
Prior art keywords
azetidinones
enantioselective synthesis
lactone based
hydroxy gamma
based enantioselective
Prior art date
Application number
ZA9704678A
Other languages
English (en)
Inventor
Guang-Zhong Wu
Yee-Shing Wong
Martin Steinman
Xing Chen
Doris P Schumacher
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
Publication of ZA974678B publication Critical patent/ZA974678B/xx

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Hematology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
ZA9704678A 1996-05-31 1997-05-28 3-Hydroxy gamma-lactone based enantioselective synthesis of azetidinones. ZA974678B (en)

Applications Claiming Priority (1)

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

Publications (1)

Publication Number Publication Date
ZA974678B true ZA974678B (en) 1997-11-28

Family

ID=24630339

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA9704678A ZA974678B (en) 1996-05-31 1997-05-28 3-Hydroxy gamma-lactone based enantioselective synthesis of azetidinones.

Country Status (14)

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

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
US6207822B1 (en) 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
ES2244238T3 (es) * 1998-12-07 2005-12-01 Schering Corporation Proceso para la sintesis de azetidinonas.
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RS20100015A (en) * 2001-01-26 2010-12-31 Schering Corporation Combination of receptor activator activated by fenofibrate peroxisome-proliferator (ppar) with sterol absorption inhibitor ezetimibe for vascular indications
US20060287254A1 (en) * 2001-01-26 2006-12-21 Schering Corporation Use of substituted azetidinone compounds for the treatment of sitosterolemia
EP1373230B1 (en) * 2001-03-28 2005-09-28 Schering Corporation Enantioselective synthesis of azetidinone intermediate compounds
DE60216300T2 (de) * 2001-09-21 2007-06-28 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
CA2517571C (en) * 2003-03-07 2011-07-05 Schering Corporation Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof
WO2004081003A1 (en) * 2003-03-07 2004-09-23 Schering Corporation Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholeterolemia
US7459442B2 (en) * 2003-03-07 2008-12-02 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
WO2005049592A1 (en) 2003-11-24 2005-06-02 Hetero Drugs Limited A novel process for ezetimibe intermediate
GB0329778D0 (en) * 2003-12-23 2004-01-28 Astrazeneca Ab Chemical compounds
EP1699759B1 (en) * 2003-12-23 2010-10-20 AstraZeneca AB Diphenylazetidinone derivates possessing cholesterol absorption inhibitory activity
WO2005069900A2 (en) * 2004-01-16 2005-08-04 Merck & Co., Inc. Npc1l1 (npc3) and methods of identifying ligands thereof
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
WO2006026273A2 (en) * 2004-08-25 2006-03-09 Merck & Co., Inc. Method of treating atherosclerosis, dyslipidemias and related conditions
US20060160785A1 (en) * 2004-12-03 2006-07-20 Judith Aronhime Ezetimibe polymorphs
US20060234996A1 (en) * 2005-04-14 2006-10-19 Itai Adin Novel crystalline form of ezetimibe and processes for the preparation thereof
US7635705B2 (en) * 2005-06-20 2009-12-22 Schering Corporation Heteroatom-linked substituted piperidines and derivatives thereof useful as histamine H3 antagonists
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
JP2008517951A (ja) * 2005-09-08 2008-05-29 テバ ファーマシューティカル インダストリーズ リミティド （３ｒ，４ｓ）−４−（（４−ベンジルオキシ）フェニル）−１−（４−フルオロフェニル）−３−（（ｓ）−３−（４−フルオロフェニル）−３−ヒドロキシプロピル）−２−アゼチジノン、すなわちエゼチミベの合成のための中間体の調製方法
CN101291662A (zh) 2005-10-21 2008-10-22 诺瓦提斯公司 肾素抑制剂和抗血脂异常剂和/或抗肥胖剂的组合
HUP0501164A2 (en) * 2005-12-20 2007-07-30 Richter Gedeon Nyrt New industrial process for the production of ezetimibe
ATE445596T1 (de) * 2005-12-22 2009-10-15 Medichem Sa Verfahren zur herstellung von zwischenprodukten für die herstellung von 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
EP2007718A2 (en) * 2006-03-29 2008-12-31 Medichem, S.A. Processes for preparing ezetimibe and intermediate compounds useful for the preparation thereof
AR060623A1 (es) * 2006-04-27 2008-07-02 Astrazeneca Ab Compuestos derivados de 2-azetidinona y un metodo de preparacion
EP1937636A1 (en) * 2006-08-29 2008-07-02 Teva Pharmaceutical Industries Ltd. Processes for the purification of (3r,4s)-4-(4-hydroxy-protected-phenyl)-1-(4-fluorophenyl)-3-(4-fluorophenyl)-3-oxopropyl¨azetidin-2-one
WO2008030382A1 (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
AU2007318058A1 (en) * 2006-11-02 2008-05-15 Merck Sharp & Dohme Corp. Heterocyclyl-substituted anti-hypercholesterolemic compounds
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 (en) * 2008-05-26 2009-12-02 Lek Pharmaceuticals D.D. Ezetimibe process and composition
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
WO2011140219A1 (en) 2010-05-04 2011-11-10 Codexis, Inc. Biocatalysts for ezetimibe synthesis
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
CA2255662A1 (en) 1997-12-04
PT906278E (pt) 2003-01-31
CA2255662C (en) 2005-11-08
EP0906278B1 (en) 2002-10-16
JPH11511754A (ja) 1999-10-12
DE69716426D1 (de) 2002-11-21
EP0906278A1 (en) 1999-04-07
ATE226191T1 (de) 2002-11-15
AU3299497A (en) 1998-01-05
CO4770966A1 (es) 1999-04-30
AR007314A1 (es) 1999-10-27
WO1997045406A1 (en) 1997-12-04
DE69716426T2 (de) 2003-08-14
US5739321A (en) 1998-04-14
ES2185026T3 (es) 2003-04-16
JP3155759B2 (ja) 2001-04-16
DK0906278T3 (da) 2003-02-17

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