AR025144A1 - Proceso para preparar azetidinonas, proceso para preparar compuestos intermediarios asi como dichos compuestos intermediarios - Google Patents
Proceso para preparar azetidinonas, proceso para preparar compuestos intermediarios asi como dichos compuestos intermediariosInfo
- Publication number
- AR025144A1 AR025144A1 ARP990106206A ARP990106206A AR025144A1 AR 025144 A1 AR025144 A1 AR 025144A1 AR P990106206 A ARP990106206 A AR P990106206A AR P990106206 A ARP990106206 A AR P990106206A AR 025144 A1 AR025144 A1 AR 025144A1
- Authority
- AR
- Argentina
- Prior art keywords
- formula
- intermediate compounds
- prepare
- azetidinones
- ketone
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 3
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 abstract 2
- 150000001408 amides Chemical class 0.000 abstract 2
- 239000003054 catalyst Substances 0.000 abstract 2
- 239000003795 chemical substances by application Substances 0.000 abstract 2
- 150000002576 ketones Chemical class 0.000 abstract 2
- 125000001181 organosilyl group Chemical group [SiH3]* 0.000 abstract 2
- JVSFQJZRHXAUGT-UHFFFAOYSA-N 2,2-dimethylpropanoyl chloride Chemical compound CC(C)(C)C(Cl)=O JVSFQJZRHXAUGT-UHFFFAOYSA-N 0.000 abstract 1
- YEFNGQDRRNBOBN-UHFFFAOYSA-N 2-(4-fluorobenzoyl)butanoic acid Chemical compound CCC(C(O)=O)C(=O)C1=CC=C(F)C=C1 YEFNGQDRRNBOBN-UHFFFAOYSA-N 0.000 abstract 1
- KRHYYFGTRYWZRS-UHFFFAOYSA-M Fluoride anion Chemical compound [F-] KRHYYFGTRYWZRS-UHFFFAOYSA-M 0.000 abstract 1
- 230000010933 acylation Effects 0.000 abstract 1
- 238000005917 acylation reaction Methods 0.000 abstract 1
- 125000003277 amino group Chemical group 0.000 abstract 1
- MNFORVFSTILPAW-UHFFFAOYSA-N azetidin-2-one Chemical class O=C1CCN1 MNFORVFSTILPAW-UHFFFAOYSA-N 0.000 abstract 1
- 230000000871 hypocholesterolemic effect Effects 0.000 abstract 1
- 150000002466 imines Chemical class 0.000 abstract 1
- 150000003951 lactams Chemical class 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 abstract 1
- 239000003223 protective agent Substances 0.000 abstract 1
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)
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US20693198A | 1998-12-07 | 1998-12-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR025144A1 true AR025144A1 (es) | 2002-11-13 |
Family
ID=22768573
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP990106206A AR025144A1 (es) | 1998-12-07 | 1999-12-06 | Proceso para preparar azetidinonas, proceso para preparar compuestos intermediarios asi como dichos compuestos intermediarios |
Country Status (13)
| Country | Link |
|---|---|
| EP (1) | EP1137634B1 (enExample) |
| JP (3) | JP3640888B2 (enExample) |
| CN (1) | CN1130342C (enExample) |
| AR (1) | AR025144A1 (enExample) |
| AT (1) | ATE297892T1 (enExample) |
| AU (1) | AU2030100A (enExample) |
| CA (1) | CA2353981C (enExample) |
| DE (1) | DE69925862T2 (enExample) |
| ES (1) | ES2244238T3 (enExample) |
| HK (1) | HK1039487B (enExample) |
| PT (1) | PT1137634E (enExample) |
| WO (1) | WO2000034240A1 (enExample) |
| ZA (1) | ZA200104004B (enExample) |
Families Citing this family (68)
| 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 |
| IL156445A0 (en) | 2001-01-26 | 2004-01-04 | Schering Corp | Combinations of peroxisome proliferator-activated receptor (ppar) activator(s) and sterol absorption inhibitor(s) and treatments for vascular indications |
| KR20070120617A (ko) | 2001-01-26 | 2007-12-24 | 쉐링 코포레이션 | 치환된 아제티딘온 화합물을 포함하는 약제학적 조성물 |
| US7071181B2 (en) | 2001-01-26 | 2006-07-04 | Schering Corporation | Methods and therapeutic combinations for the treatment of diabetes using sterol absorption inhibitors |
| BRPI0208384B1 (pt) | 2001-03-28 | 2016-05-31 | Merck Sharp & Dohme | síntese enantiosseletiva de compostos intermediários de azetidinona |
| EP1429756B1 (en) | 2001-09-21 | 2006-11-22 | Schering Corporation | Treatment of xanthoma with azetidinone derivatives as 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 |
| US7053080B2 (en) | 2001-09-21 | 2006-05-30 | Schering Corporation | Methods and therapeutic combinations for the treatment of obesity using sterol absorption inhibitors |
| 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 |
| CA2504916A1 (en) | 2002-11-06 | 2004-05-27 | Schering Corporation | Cholesterol absorptions inhibitors for the treatment of autoimmune disorders |
| US7459442B2 (en) | 2003-03-07 | 2008-12-02 | Schering Corporation | Substituted azetidinone compounds, processes for preparing the same, formulations and uses thereof |
| WO2004081004A1 (en) | 2003-03-07 | 2004-09-23 | Schering Corporation | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia |
| DE602004018617D1 (de) | 2003-03-07 | 2009-02-05 | Schering Corp | Substituierte azetidinon-derivate, deren pharmazeutische formulierungen und deren verwendung zur behandlung von hypercholesterolemia |
| WO2004081002A1 (en) | 2003-03-07 | 2004-09-23 | Schering Corporation | Substituted azetidinone compounds, formulations and uses thereof for the treatment of hypercholesterolemia |
| 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 |
| 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 |
| AU2006244043A1 (en) * | 2005-05-11 | 2006-11-16 | Microbia, Inc. | Processes for production of phenolic 4-biphenylylazetidin-2-ones |
| EA200702614A1 (ru) * | 2005-05-25 | 2008-04-28 | Майкробиа, Инк. | Способы получения 4-(бифенилил)азетидин-2-оналкилфосфиновых кислот |
| 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 |
| RU2008119687A (ru) | 2005-10-21 | 2009-11-27 | Новартис АГ (CH) | Комбинации органических соединений |
| HU0501164D0 (en) * | 2005-12-20 | 2006-02-28 | Richter Gedeon Vegyeszet | New industrial process for the production of ezetimibe |
| CN101384532B (zh) * | 2006-02-16 | 2013-01-02 | 寿制药株式会社 | 制造光学活性醇的方法 |
| US7910698B2 (en) | 2006-02-24 | 2011-03-22 | Schering Corporation | NPC1L1 orthologues |
| AR060623A1 (es) | 2006-04-27 | 2008-07-02 | Astrazeneca Ab | Compuestos derivados de 2-azetidinona y un metodo de preparacion |
| 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 |
| EP2414529A2 (en) | 2009-04-01 | 2012-02-08 | 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 |
| MX392182B (es) | 2015-03-13 | 2025-03-21 | 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 |
| 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 |
| CN117843543B (zh) * | 2024-01-02 | 2026-06-19 | 南京工业大学 | 一种α,α-二氟丙内酰胺的制备方法 |
Family Cites Families (5)
| 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 |
| PT707567E (pt) * | 1993-07-09 | 2002-01-30 | Schering Corp | Processo de sintese de azetidinonas |
| US5631365A (en) * | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
| AU7472896A (en) * | 1995-11-02 | 1997-05-22 | Schering Corporation | Process for preparing 1-(4-fluorophenyl)-3(r)-(3(s)-hydroxy-3-({phenyl or 4-fluorophenyl})-propyl)-4(s)-(4-hydroxyphenyl)-2-azetidinon |
| US5739321A (en) * | 1996-05-31 | 1998-04-14 | Schering Corporation | 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones |
-
1999
- 1999-12-06 CA CA002353981A patent/CA2353981C/en not_active Expired - Fee Related
- 1999-12-06 ES ES99963973T patent/ES2244238T3/es not_active Expired - Lifetime
- 1999-12-06 AU AU20301/00A patent/AU2030100A/en not_active Abandoned
- 1999-12-06 AT AT99963973T patent/ATE297892T1/de active
- 1999-12-06 HK HK02100567.1A patent/HK1039487B/en not_active IP Right Cessation
- 1999-12-06 JP JP2000586688A patent/JP3640888B2/ja not_active Expired - Lifetime
- 1999-12-06 WO PCT/US1999/027914 patent/WO2000034240A1/en not_active Ceased
- 1999-12-06 EP EP99963973A patent/EP1137634B1/en not_active Expired - Lifetime
- 1999-12-06 DE DE69925862T patent/DE69925862T2/de not_active Expired - Lifetime
- 1999-12-06 CN CN99814140A patent/CN1130342C/zh not_active Expired - Lifetime
- 1999-12-06 PT PT99963973T patent/PT1137634E/pt unknown
- 1999-12-06 AR ARP990106206A patent/AR025144A1/es not_active Application Discontinuation
-
2001
- 2001-05-16 ZA ZA200104004A patent/ZA200104004B/en unknown
-
2004
- 2004-11-09 JP JP2004325744A patent/JP4616620B2/ja not_active Expired - Lifetime
-
2010
- 2010-09-27 JP JP2010216153A patent/JP2011016841A/ja not_active Withdrawn
Also Published As
| Publication number | Publication date |
|---|---|
| ZA200104004B (en) | 2002-08-16 |
| JP4616620B2 (ja) | 2011-01-19 |
| CA2353981A1 (en) | 2000-06-15 |
| EP1137634B1 (en) | 2005-06-15 |
| EP1137634A1 (en) | 2001-10-04 |
| WO2000034240A1 (en) | 2000-06-15 |
| HK1039487A1 (en) | 2002-04-26 |
| JP2002531546A (ja) | 2002-09-24 |
| ES2244238T3 (es) | 2005-12-01 |
| PT1137634E (pt) | 2005-10-31 |
| HK1039487B (en) | 2005-08-12 |
| JP3640888B2 (ja) | 2005-04-20 |
| CN1130342C (zh) | 2003-12-10 |
| JP2005053931A (ja) | 2005-03-03 |
| AU2030100A (en) | 2000-06-26 |
| CA2353981C (en) | 2005-04-26 |
| ATE297892T1 (de) | 2005-07-15 |
| DE69925862T2 (de) | 2006-05-04 |
| DE69925862D1 (de) | 2005-07-21 |
| CN1329592A (zh) | 2002-01-02 |
| JP2011016841A (ja) | 2011-01-27 |
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