JP2005053931A5 - - Google Patents

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Publication number
JP2005053931A5
JP2005053931A5 JP2004325744A JP2004325744A JP2005053931A5 JP 2005053931 A5 JP2005053931 A5 JP 2005053931A5 JP 2004325744 A JP2004325744 A JP 2004325744A JP 2004325744 A JP2004325744 A JP 2004325744A JP 2005053931 A5 JP2005053931 A5 JP 2005053931A5
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JP
Japan
Prior art keywords
phenyl
alkyl
naphthyl
protecting group
hydroxy protecting
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.)
Granted
Application number
JP2004325744A
Other languages
English (en)
Japanese (ja)
Other versions
JP4616620B2 (ja
JP2005053931A (ja
Filing date
Publication date
Application filed filed Critical
Publication of JP2005053931A publication Critical patent/JP2005053931A/ja
Publication of JP2005053931A5 publication Critical patent/JP2005053931A5/ja
Application granted granted Critical
Publication of JP4616620B2 publication Critical patent/JP4616620B2/ja
Anticipated expiration legal-status Critical
Expired - Lifetime legal-status Critical Current

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JP2004325744A 1998-12-07 2004-11-09 アゼチジノンの合成プロセス Expired - Lifetime JP4616620B2 (ja)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US20693198A 1998-12-07 1998-12-07

Related Parent Applications (1)

Application Number Title Priority Date Filing Date
JP2000586688A Division JP3640888B2 (ja) 1998-12-07 1999-12-06 アゼチジノンの合成プロセス

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2010216153A Division JP2011016841A (ja) 1998-12-07 2010-09-27 アゼチジノンの合成プロセス

Publications (3)

Publication Number Publication Date
JP2005053931A JP2005053931A (ja) 2005-03-03
JP2005053931A5 true JP2005053931A5 (enExample) 2007-01-25
JP4616620B2 JP4616620B2 (ja) 2011-01-19

Family

ID=22768573

Family Applications (3)

Application Number Title Priority Date Filing Date
JP2000586688A Expired - Lifetime JP3640888B2 (ja) 1998-12-07 1999-12-06 アゼチジノンの合成プロセス
JP2004325744A Expired - Lifetime JP4616620B2 (ja) 1998-12-07 2004-11-09 アゼチジノンの合成プロセス
JP2010216153A Withdrawn JP2011016841A (ja) 1998-12-07 2010-09-27 アゼチジノンの合成プロセス

Family Applications Before (1)

Application Number Title Priority Date Filing Date
JP2000586688A Expired - Lifetime JP3640888B2 (ja) 1998-12-07 1999-12-06 アゼチジノンの合成プロセス

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2010216153A Withdrawn JP2011016841A (ja) 1998-12-07 2010-09-27 アゼチジノンの合成プロセス

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)

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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)

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US5561227A (en) * 1991-07-23 1996-10-01 Schering Corporation Process for the stereospecific synthesis of azetidinones
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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

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