HK1039487B - Process for the synthesis of azetidinones - Google Patents

Process for the synthesis of azetidinones Download PDF

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Publication number
HK1039487B
HK1039487B HK02100567.1A HK02100567A HK1039487B HK 1039487 B HK1039487 B HK 1039487B HK 02100567 A HK02100567 A HK 02100567A HK 1039487 B HK1039487 B HK 1039487B
Authority
HK
Hong Kong
Prior art keywords
formula
phenyl
substituted
agent
alkyl
Prior art date
Application number
HK02100567.1A
Other languages
German (de)
English (en)
French (fr)
Chinese (zh)
Other versions
HK1039487A1 (en
Inventor
K. Thiruvengadam Tiruvettipuram
Fu Xiaoyong
Tann Chou-Hong
L. Mcallister Timothy
S. Chiu John
Colon Cesar
Original Assignee
Merck Sharp & Dohme 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
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=22768573&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=HK1039487(B) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Merck Sharp & Dohme Corp. filed Critical Merck Sharp & Dohme Corp.
Publication of HK1039487A1 publication Critical patent/HK1039487A1/en
Publication of HK1039487B publication Critical patent/HK1039487B/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
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Catalysts (AREA)
HK02100567.1A 1998-12-07 1999-12-06 Process for the synthesis of azetidinones HK1039487B (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20693198A 1998-12-07 1998-12-07
US09/206931 1998-12-07
PCT/US1999/027914 WO2000034240A1 (en) 1998-12-07 1999-12-06 Process for the synthesis of azetidinones

Publications (2)

Publication Number Publication Date
HK1039487A1 HK1039487A1 (en) 2002-04-26
HK1039487B true HK1039487B (en) 2005-08-12

Family

ID=22768573

Family Applications (1)

Application Number Title Priority Date Filing Date
HK02100567.1A HK1039487B (en) 1998-12-07 1999-12-06 Process for the synthesis of azetidinones

Country Status (13)

Country Link
EP (1) EP1137634B1 (https=)
JP (3) JP3640888B2 (https=)
CN (1) CN1130342C (https=)
AR (1) AR025144A1 (https=)
AT (1) ATE297892T1 (https=)
AU (1) AU2030100A (https=)
CA (1) CA2353981C (https=)
DE (1) DE69925862T2 (https=)
ES (1) ES2244238T3 (https=)
HK (1) HK1039487B (https=)
PT (1) PT1137634E (https=)
WO (1) WO2000034240A1 (https=)
ZA (1) ZA200104004B (https=)

Families Citing this family (68)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6982251B2 (en) 2000-12-20 2006-01-03 Schering Corporation Substituted 2-azetidinones useful as hypocholesterolemic agents
DK1355644T3 (da) 2001-01-26 2006-10-23 Schering Corp Anvendelse af substituerede azetidinonforbindelser til behandling af sitosterolæmi
US7071181B2 (en) 2001-01-26 2006-07-04 Schering Corporation Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors
HU230253B1 (hu) 2001-01-26 2015-11-30 Merck Sharp & Dohme Corp Peroxiszóma proliferátor-aktivált receptor (PPAR) aktivátor(ok) és szterin-abszorpció inhibitor(ok) kombinációi és alkalmazásuk vaszkuláris indikációk kezelésére
DK1373230T3 (da) 2001-03-28 2005-11-07 Schering Corp Enantiselektiv syntese af azetidinon mellemprodukter
US7053080B2 (en) 2001-09-21 2006-05-30 Schering Corporation Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors
US7056906B2 (en) 2001-09-21 2006-06-06 Schering Corporation Combinations of hormone replacement therapy composition(s) and sterol absorption inhibitor(s) and treatments for vascular conditions in post-menopausal women
JP2005504091A (ja) 2001-09-21 2005-02-10 シェーリング　コーポレイション ステロール吸収阻害剤としてアゼチジノンを用いる黄色腫の処置
WO2003104180A1 (en) * 2002-06-05 2003-12-18 Natco Pharma Limited Process for the preparation of 4-(4-fluorobenzoyl) butyric acid
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
WO2004043457A1 (en) 2002-11-06 2004-05-27 Schering Corporation Cholesterol absorptions inhibitors for the treatment of autoimmune disorders
JP4589919B2 (ja) 2003-03-07 2010-12-01 シェーリング コーポレイション 高コレステロール血症の処置のための、置換アゼチジノン化合物、これらの処方物および使用
CA2517571C (en) 2003-03-07 2011-07-05 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
JP2006519869A (ja) 2003-03-07 2006-08-31 シェーリング　コーポレイション 置換アゼチジノン化合物、置換アゼチジノン化合物を調製するためのプロセス、それらの処方物および使用
AR041089A1 (es) 2003-05-15 2005-05-04 Merck & Co Inc Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas
AU2003282384A1 (en) 2003-11-24 2005-06-08 Hetero Drugs Limited A novel process for ezetimibe intermediate
ATE485267T1 (de) 2003-12-23 2010-11-15 Astrazeneca Ab Diphenylazetidinonderivate mit die cholesterinabsorption hemmender wirkung
JP4590417B2 (ja) 2004-01-16 2010-12-01 メルク・シャープ・エンド・ドーム・コーポレイション Ｎｐｃ１ｌ１（ｎｐｃ３）およびこのリガンドの同定方法
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
WO2006050634A1 (en) * 2004-11-15 2006-05-18 Xiamen Mchem Pharma (Group) Ltd. A preparation method of 1-(4-fluorophenyl)-(3r)-[3-(4-fluorophenyl)-(3s)-hydroxypropyl]-(4s)-(4-hydroxyphenyl)-2-azetidinone
EP1831162B1 (en) 2004-12-20 2012-10-31 Merck Sharp & Dohme Corp. Process for the synthesis of azetidinones
TW200726746A (en) * 2005-05-06 2007-07-16 Microbia Inc Processes for production of 4-biphenylylazetidin-2-ones
MX2007014172A (es) * 2005-05-11 2008-04-02 Microbia Inc Procedimiento para la produccion de 4-bifenililacetidina-2-onas fenolicos.
JP2008545700A (ja) * 2005-05-25 2008-12-18 マイクロビア インコーポレーテッド ４−（ビフェニリル）アゼチジン−２−オンホスホン酸類の製造方法
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
WO2007017705A1 (en) * 2005-08-09 2007-02-15 Glenmark Pharmaceuticals Limited Process for the preparation of azetidinones
JP2009512715A (ja) 2005-10-21 2009-03-26 ノバルティス アクチエンゲゼルシャフト レニン阻害剤と抗異脂肪血症剤および／または抗肥満症剤の組み合わせ
HUP0501164A2 (en) * 2005-12-20 2007-07-30 Richter Gedeon Nyrt New industrial process for the production of ezetimibe
MX2008010235A (es) 2006-02-16 2008-10-23 Kotobuki Pharmaceutical Co Ltd Metodo para producir alcohol opticamente activo.
US7910698B2 (en) 2006-02-24 2011-03-22 Schering Corporation NPC1L1 orthologues
TW200811098A (en) 2006-04-27 2008-03-01 Astrazeneca Ab Chemical compounds
CN100564357C (zh) * 2006-10-20 2009-12-02 浙江天宇药业有限公司 一种氮杂环丁酮衍生物及其合成方法
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
AR074752A1 (es) * 2008-12-17 2011-02-09 Hanmi Pharm Ind Co Ltd Metodo para preparar ezetimiba e intermediarios usados en la misma
WO2010113175A2 (en) 2009-04-01 2010-10-07 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
WO2010141494A2 (en) * 2009-06-02 2010-12-09 Codexis, Inc. Synthesis of ezetimibe
CN101935309B (zh) * 2009-06-29 2013-11-13 上海特化医药科技有限公司 依泽替米贝的制备方法及其中间体
CN101845010B (zh) * 2010-02-10 2012-07-25 浙江大学 一种制备伊替米贝的方法
ES2372460B1 (es) 2010-07-09 2012-11-16 Moehs Ibérica S.L. Nuevo método para la preparación de ezetimiba.
WO2012076030A1 (en) * 2010-12-10 2012-06-14 Pharmathen S.A. Process for the preparation of intermediate compounds useful in the preparation of ezetimibe
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
CN103102297A (zh) * 2012-09-28 2013-05-15 北京赛林泰医药技术有限公司 一种新的依折麦布的合成方法
CN103864708A (zh) * 2012-12-12 2014-06-18 天津市医药集团技术发展有限公司 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
CN103819382A (zh) * 2014-01-01 2014-05-28 北京万全德众医药生物技术有限公司 一种依折麦布杂质的制备方法
CN103965089B (zh) * 2014-04-18 2016-06-29 上海方楠生物科技有限公司 一种立体选择性的合成降血脂药物依折麦布的方法
CN104230978B (zh) * 2014-09-22 2016-09-28 上海现代制药股份有限公司 依折麦布的制备中间体及其制备方法
CN104447474A (zh) * 2014-11-11 2015-03-25 武汉武药科技有限公司 一种依折麦布异构体的合成方法
CN104402790B (zh) * 2014-12-28 2016-09-28 严白双 一种制备依折麦布的改进工艺
EP3267989A4 (en) 2015-03-13 2018-11-07 Esperion Therapeutics, Inc. Fixed dose combinations and formulations comprising etc1002 and ezetimibe and methods of treating or reducing the risk of cardiovascular disease
MA41793A (fr) 2015-03-16 2018-01-23 Esperion Therapeutics Inc Associations de doses fixes comprenant du etc1002 et une ou plusieurs statines permettant de traiter ou de réduire un risque cardiovasculaire
CN104892537B (zh) * 2015-05-15 2018-07-17 江西施美药业股份有限公司 依折麦布中间体以及依折麦布的合成方法
CN104829511A (zh) * 2015-05-18 2015-08-12 广州南新制药有限公司 一种依折麦布的合成工艺
CN105237492A (zh) * 2015-10-29 2016-01-13 无锡福祈制药有限公司 一种依折麦布中间体的合成方法
CN105524010B (zh) * 2015-12-16 2018-10-26 江苏恒盛药业有限公司 一种依泽麦布中间体及其制备方法
CN105566243B (zh) * 2016-01-15 2017-10-31 齐鲁天和惠世制药有限公司 从依折麦布生产废液中回收(s)‑(+)‑4‑苯基‑2‑噁唑烷酮的方法
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
JP6711709B2 (ja) * 2016-05-10 2020-06-17 株式会社トクヤマ エゼチミブの製造方法
CN106967106B (zh) * 2017-04-24 2018-08-10 上海华源医药科技发展有限公司 一种依折麦布中间体的生产方法
JP6802121B2 (ja) 2017-08-04 2020-12-16 株式会社シマノ 自転車用コンポーネント
CN110818606B (zh) * 2018-08-08 2021-06-29 上海博志研新药物技术有限公司 依折麦布及其中间体的制备方法
CN112441959A (zh) * 2020-12-07 2021-03-05 石家庄市华新药业有限责任公司 一种依折麦布原料药合成工艺
CN115850144A (zh) * 2022-12-30 2023-03-28 湖南方盛绿色合成制药有限公司 依折麦布的制备工艺
CN116283948A (zh) * 2023-02-24 2023-06-23 江苏阿尔法药业股份有限公司 一种依折麦布中间体的合成方法
CN117843543A (zh) * 2024-01-02 2024-04-09 南京工业大学 一种α,α-二氟丁内酰胺的制备方法

Family Cites Families (5)

* 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
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
US5739321A (en) * 1996-05-31 1998-04-14 Schering Corporation 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones

Also Published As

Publication number Publication date
AU2030100A (en) 2000-06-26
JP4616620B2 (ja) 2011-01-19
JP2002531546A (ja) 2002-09-24
HK1039487A1 (en) 2002-04-26
DE69925862T2 (de) 2006-05-04
JP3640888B2 (ja) 2005-04-20
CN1130342C (zh) 2003-12-10
JP2011016841A (ja) 2011-01-27
DE69925862D1 (de) 2005-07-21
CN1329592A (zh) 2002-01-02
CA2353981A1 (en) 2000-06-15
AR025144A1 (es) 2002-11-13
ZA200104004B (en) 2002-08-16
CA2353981C (en) 2005-04-26
PT1137634E (pt) 2005-10-31
ES2244238T3 (es) 2005-12-01
JP2005053931A (ja) 2005-03-03
WO2000034240A1 (en) 2000-06-15
ATE297892T1 (de) 2005-07-15
EP1137634B1 (en) 2005-06-15
EP1137634A1 (en) 2001-10-04

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