ES2524086T3 - Nuevo método para la preparación de ezetimiba - Google Patents

Nuevo método para la preparación de ezetimiba Download PDF

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Publication number
ES2524086T3
ES2524086T3 ES11738419.8T ES11738419T ES2524086T3 ES 2524086 T3 ES2524086 T3 ES 2524086T3 ES 11738419 T ES11738419 T ES 11738419T ES 2524086 T3 ES2524086 T3 ES 2524086T3
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ES
Spain
Prior art keywords
formula
ezetimibe
preparation
new method
compound
Prior art date
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Active
Application number
ES11738419.8T
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English (en)
Inventor
Carles SÁNCHEZ CASALS
Alicia DOBARRO RODRÍGUEZ
Juan Bosch Cartes
Davinia GARCÍA DÍAZ
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.)
Moehs Iberica SL
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Moehs Iberica SL
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Application granted granted Critical
Publication of ES2524086T3 publication Critical patent/ES2524086T3/es
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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/16—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D263/18—Oxygen atoms
    • C07D263/20—Oxygen atoms attached in position 2
    • C07D263/26—Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom

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)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

Método para la preparación de ezetimiba (7) que comprende las siguientes etapas: (a) hacer reaccionar un compuesto de fórmula (1) **Fórmula** donde Ph representa un grupo fenilo y Prot representa un grupo protector de hidroxilos, con una imina de fórmula(2) **Fórmula** para dar una mezcla diastereoisomérica (3a) y (3b) cuyo producto mayoritario es el compuesto de fórmula (3a), **Fórmula**

Description

5
50
ES11738419.8T 2010-07-09 2011-07-08 Nuevo método para la preparación de ezetimiba Active ES2524086T3 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
ES201031052A ES2372460B1 (es) 2010-07-09 2010-07-09 Nuevo método para la preparación de ezetimiba.
ES201031052 2010-07-09
PCT/EP2011/061616 WO2012004382A1 (en) 2010-07-09 2011-07-08 New method for preparing ezetimibe

Publications (1)

Publication Number Publication Date
ES2524086T3 true ES2524086T3 (es) 2014-12-04

Family

ID=44532780

Family Applications (2)

Application Number Title Priority Date Filing Date
ES201031052A Expired - Fee Related ES2372460B1 (es) 2010-07-09 2010-07-09 Nuevo método para la preparación de ezetimiba.
ES11738419.8T Active ES2524086T3 (es) 2010-07-09 2011-07-08 Nuevo método para la preparación de ezetimiba

Family Applications Before (1)

Application Number Title Priority Date Filing Date
ES201031052A Expired - Fee Related ES2372460B1 (es) 2010-07-09 2010-07-09 Nuevo método para la preparación de ezetimiba.

Country Status (5)

Country Link
EP (1) EP2590940B1 (es)
ES (2) ES2372460B1 (es)
HR (1) HRP20141061T1 (es)
SI (1) SI2590940T1 (es)
WO (1) WO2012004382A1 (es)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN102746249B (zh) * 2012-07-07 2013-12-25 山东诚创医药技术开发有限公司 一种依折麦布中间体的纯化精制方法
CN103450084B (zh) * 2013-09-09 2015-01-28 厦门大学 除草剂异丙吡草酯的制备方法
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
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

Family Cites Families (12)

* 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
US5739321A (en) 1996-05-31 1998-04-14 Schering Corporation 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
JP3640888B2 (ja) 1998-12-07 2005-04-20 シェーリング コーポレイション アゼチジノンの合成プロセス
JP2001209500A (ja) * 2000-01-28 2001-08-03 Fujitsu Ltd ディスク装置およびディスク装置のリード・ライト処理方法
BR0116325A (pt) * 2000-12-21 2003-10-14 Aventis Pharma Gmbh 1,2-difenilazetidinonas, processos para a sua preparação, medicamentos contendo estes compostos e sua aplicação para o tratamento de distúrbios do metabolismo de lipìdios
DE102005055726A1 (de) * 2005-11-23 2007-08-30 Sanofi-Aventis Deutschland Gmbh Hydroxy-substituierte Diphenylazetidinone, Verfahren zu deren Herstellung, diese Verbindungen enthaltende Arzneimittel und deren Verwendung
HU0501164D0 (en) * 2005-12-20 2006-02-28 Richter Gedeon Vegyeszet New industrial process for the production of ezetimibe
DE602006009845D1 (de) 2005-12-22 2009-11-26 Medichem Sa Verfahren zur herstellung von zwischenprodukten für die herstellung von ezetimibe
CZ302395B6 (cs) 2007-03-02 2011-04-27 Zentiva, A. S. Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu
CZ2008317A3 (cs) * 2008-05-21 2009-12-02 Zentiva, A. S. Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu
WO2010141494A2 (en) * 2009-06-02 2010-12-09 Codexis, Inc. Synthesis of ezetimibe

Also Published As

Publication number Publication date
WO2012004382A1 (en) 2012-01-12
ES2372460A1 (es) 2012-01-20
ES2372460B1 (es) 2012-11-16
SI2590940T1 (sl) 2014-12-31
HRP20141061T1 (hr) 2015-01-02
EP2590940A1 (en) 2013-05-15
EP2590940B1 (en) 2014-08-27

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