DE69925862D1 - Verfahren zur herstellung von azetidinonen - Google Patents

Verfahren zur herstellung von azetidinonen

Info

Publication number
DE69925862D1
DE69925862D1 DE69925862T DE69925862T DE69925862D1 DE 69925862 D1 DE69925862 D1 DE 69925862D1 DE 69925862 T DE69925862 T DE 69925862T DE 69925862 T DE69925862 T DE 69925862T DE 69925862 D1 DE69925862 D1 DE 69925862D1
Authority
DE
Germany
Prior art keywords
azetidinones
production
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
DE69925862T
Other languages
English (en)
Other versions
DE69925862T2 (de
Inventor
Tiruvettipuram K Thiruvengadam
Xiaoyong Fu
Chou-Hong Tann
Timothy L Mcallister
John S Chiu
Cesar Colon
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
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=DE69925862(D1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Application granted granted Critical
Publication of DE69925862D1 publication Critical patent/DE69925862D1/de
Publication of DE69925862T2 publication Critical patent/DE69925862T2/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
    • 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)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Catalysts (AREA)
  • Plural Heterocyclic Compounds (AREA)
DE69925862T 1998-12-07 1999-12-06 Verfahren zur herstellung von azetidinonen Expired - Lifetime DE69925862T2 (de)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US20693198A 1998-12-07 1998-12-07
US206931 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
DE69925862D1 true DE69925862D1 (de) 2005-07-21
DE69925862T2 DE69925862T2 (de) 2006-05-04

Family

ID=22768573

Family Applications (1)

Application Number Title Priority Date Filing Date
DE69925862T Expired - Lifetime DE69925862T2 (de) 1998-12-07 1999-12-06 Verfahren zur herstellung von azetidinonen

Country Status (13)

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

Families Citing this family (53)

* Cited by examiner, † Cited by third party
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SI1373230T1 (sl) 2001-03-28 2005-12-31 Schering Corp Enantioselektivna sinteza azetidinonskih intermediatnih spojin
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
AR041089A1 (es) 2003-05-15 2005-05-04 Merck & Co Inc Procedimiento y composiciones farmaceutiicas para tratar aterosclerosis, dislipidemias y afecciones relacionadas
US7067675B2 (en) 2003-11-24 2006-06-27 Hetero Drugs Limited Process for ezetimibe intermediate
DE602004029715D1 (de) 2003-12-23 2010-12-02 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
WO2006050634A1 (fr) * 2004-11-15 2006-05-18 Xiamen Mchem Pharma (Group) Ltd. Procede de preparation de la 1-(4-fluorophenyl)-(3r)-[3-(4-fluorophenyl)-(3s)-hydroxypropyl]-(4s)-(4-hydroxyphenyl)-2-azetidinone
US20060135755A1 (en) * 2004-12-20 2006-06-22 Schering Corporation Process for the synthesis of azetidinones
TW200726746A (en) * 2005-05-06 2007-07-16 Microbia Inc Processes for production of 4-biphenylylazetidin-2-ones
KR20080017345A (ko) * 2005-05-11 2008-02-26 마이크로비아 인코포레이티드 페놀성 4-비페닐일아제티딘-2-온의 제조방법
KR20080025077A (ko) * 2005-05-25 2008-03-19 마이크로비아 인코포레이티드 4-(비페닐일)아제티딘-2-온 포스폰산의 제조방법
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
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
HU0501164D0 (en) * 2005-12-20 2006-02-28 Richter Gedeon Vegyeszet New industrial process for the production of ezetimibe
KR101074968B1 (ko) 2006-02-16 2011-10-18 고토부키 세이야쿠 가부시키가이샤 광학활성 알코올을 제조하는 방법
EP1986489A2 (de) 2006-02-24 2008-11-05 Schering Corporation Npc1l1-orthologe
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
MX2017011499A (es) 2015-03-13 2018-03-26 Esperion Therapeutics Inc Combinaciones de dosis fija y formulaciones que comprenden ácido 8-hidroxi-2,2,14,14 tetrametilpentadecanodioico (etc1002) y ezetimiba y métodos para tratar o reducir el riesgo de enfermedad cardiovascular.
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
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
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

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
DK0707567T3 (da) * 1993-07-09 2001-11-26 Schering Corp Fremgangsmåde til syntese af azetidinoner
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
WO2000034240A1 (en) 2000-06-15
HK1039487B (zh) 2005-08-12
JP2011016841A (ja) 2011-01-27
CA2353981C (en) 2005-04-26
JP2005053931A (ja) 2005-03-03
AR025144A1 (es) 2002-11-13
PT1137634E (pt) 2005-10-31
JP3640888B2 (ja) 2005-04-20
CN1329592A (zh) 2002-01-02
CA2353981A1 (en) 2000-06-15
EP1137634B1 (de) 2005-06-15
AU2030100A (en) 2000-06-26
ZA200104004B (en) 2002-08-16
HK1039487A1 (en) 2002-04-26
ES2244238T3 (es) 2005-12-01
JP4616620B2 (ja) 2011-01-19
EP1137634A1 (de) 2001-10-04
DE69925862T2 (de) 2006-05-04
ATE297892T1 (de) 2005-07-15
CN1130342C (zh) 2003-12-10
JP2002531546A (ja) 2002-09-24

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8363 Opposition against the patent
8365 Fully valid after opposition proceedings