[go: up one dir, main page]

WO2010071358A3 - Procédé de préparation d'ézétimibe et intermédiaires utilisés dans ce dernier - Google Patents

Procédé de préparation d'ézétimibe et intermédiaires utilisés dans ce dernier Download PDF

Info

Publication number
WO2010071358A3
WO2010071358A3 PCT/KR2009/007535 KR2009007535W WO2010071358A3 WO 2010071358 A3 WO2010071358 A3 WO 2010071358A3 KR 2009007535 W KR2009007535 W KR 2009007535W WO 2010071358 A3 WO2010071358 A3 WO 2010071358A3
Authority
WO
WIPO (PCT)
Prior art keywords
intermediates used
ezetimibe
preparing ezetimibe
preparing
preventing
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.)
Ceased
Application number
PCT/KR2009/007535
Other languages
English (en)
Other versions
WO2010071358A2 (fr
Inventor
Gi Jeong Kim
Choong Hahn Kim
Ji Yeon Chang
Nam Du Kim
Young Kil Chang
Gwan Sun Lee
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.)
Hanmi Pharmaceutical Co Ltd
Hanmi Pharmaceutical Industries Co Ltd
Original Assignee
Hanmi Pharmaceutical Co Ltd
Hanmi Pharmaceutical Industries Co Ltd
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
Application filed by Hanmi Pharmaceutical Co Ltd, Hanmi Pharmaceutical Industries Co Ltd filed Critical Hanmi Pharmaceutical Co Ltd
Publication of WO2010071358A2 publication Critical patent/WO2010071358A2/fr
Publication of WO2010071358A3 publication Critical patent/WO2010071358A3/fr
Anticipated expiration legal-status Critical
Ceased 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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Veterinary Medicine (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Urology & Nephrology (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La présente invention concerne un procédé de préparation d'ézétimibe qui est efficace pour prévenir ou traiter l'artériosclérose et de nouveaux intermédiaires utilisés dans ledit procédé de préparation. Selon le procédé qui ne fait pas appel à des réactifs coûteux, on peut éliminer aisément les diastéréoisomères indésirables, au moyen d'une procédure étape par étape et on peut préparer l'ézétimibe de formule 1 à un rendement élevé sans utiliser une procédure d'hydrogénation dans des conditions de pression élevée.
PCT/KR2009/007535 2008-12-17 2009-12-16 Procédé de préparation d'ézétimibe et intermédiaires utilisés dans ce dernier Ceased WO2010071358A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR10-2008-0128457 2008-12-17
KR20080128457 2008-12-17

Publications (2)

Publication Number Publication Date
WO2010071358A2 WO2010071358A2 (fr) 2010-06-24
WO2010071358A3 true WO2010071358A3 (fr) 2010-09-10

Family

ID=42269242

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2009/007535 Ceased WO2010071358A2 (fr) 2008-12-17 2009-12-16 Procédé de préparation d'ézétimibe et intermédiaires utilisés dans ce dernier

Country Status (4)

Country Link
KR (1) KR101156588B1 (fr)
AR (1) AR074752A1 (fr)
TW (1) TW201028374A (fr)
WO (1) WO2010071358A2 (fr)

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2414529A2 (fr) 2009-04-01 2012-02-08 Matrix Laboratories Ltd Procédé enzymatique pour la préparation de la (s)-5-(4-fluorophényl)-5-hydroxy-1-morpholin-4-yl-pentan-1-one, un intermédiaire de l'ézétimibe et la conversion ultérieure en ézétimibe
WO2012076030A1 (fr) 2010-12-10 2012-06-14 Pharmathen S.A. Procédé de préparation de composés intermédiaires utiles dans la préparation de l'ézétimibe
CN103086938A (zh) * 2011-10-28 2013-05-08 沈阳药科大学 依泽替米贝的合成方法
CN103204795B (zh) * 2012-01-11 2016-12-14 重庆华邦胜凯制药有限公司 一种手性氮杂环丁酮类化合物的制备方法
CN103373970A (zh) * 2012-04-16 2013-10-30 重庆圣华曦药业股份有限公司 一种依折麦布中间体的合成方法
CN106831522B (zh) * 2015-12-03 2021-06-08 中国科学院上海有机化学研究所 内酰胺类化合物及其制备方法
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
KR102078158B1 (ko) 2018-02-21 2020-02-17 강원대학교산학협력단 에제티미브의 제조방법 및 그 중간체
US11110444B2 (en) 2019-12-30 2021-09-07 Industrial Technology Research Institute Chiral catalyst and heterogeneous chiral catalyst comprising the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
WO2007072088A1 (fr) * 2005-12-20 2007-06-28 Richter Gedeon Nyrt. Procede pour la production d'ezetimibe et intermediaires utilises dans ce procede

Family Cites Families (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
CA2616058A1 (fr) * 2005-09-08 2007-03-15 Vinod Kumar Kansal Procedes pour preparer (3r,4s)-4-((4-benzyloxy)phenyle)-1-(4-fluorophenyle)-3-((s)-3-(4-fluorophenyle)-3-hydroxypropyle)-2-azetidinone, un intermediaire pour la synthese de l'ezetimibe

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5886171A (en) * 1996-05-31 1999-03-23 Schering Corporation 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
WO2007072088A1 (fr) * 2005-12-20 2007-06-28 Richter Gedeon Nyrt. Procede pour la production d'ezetimibe et intermediaires utilises dans ce procede

Also Published As

Publication number Publication date
TW201028374A (en) 2010-08-01
WO2010071358A2 (fr) 2010-06-24
KR20100070305A (ko) 2010-06-25
AR074752A1 (es) 2011-02-09
KR101156588B1 (ko) 2012-06-20

Similar Documents

Publication Publication Date Title
WO2010071358A3 (fr) Procédé de préparation d'ézétimibe et intermédiaires utilisés dans ce dernier
ZA201008121B (en) Substituted 1-(diazinyl) pyrazole-4-yl-acetic acids,method for the production thereof,and use thereof as herbicides and plant growth regulators
EP2762492A3 (fr) Procédé pour produire une préparation d'immunoglobuline hautement concentrée pour usage sous-cutané
WO2009141718A3 (fr) Procédé de préparation d'analogues de la prostaglandine et de leurs intermédiaires
WO2006092213A8 (fr) Pyrazolylcarboxanilides
UA105897C2 (uk) Спосіб покращення врожайності і/або покращення сили рослини і/або збільшення стійкості або опірності рослини до кліматичних факторів стресу за допомогою амідної сполуки та її застосування
MX2010002836A (es) Bortezomib y proceso para la produccion del mismo.
EP1961847A4 (fr) Fibre de carbone, procede de fabrication d'une fibre precurseur a base de polyacrylonitrile pour la fabrication d'une fibre de carbone et procede de fabrication d'une fibre de carbone
SG170729A1 (en) Processes and intermediates for preparing steric compounds
ZA200901254B (en) Novel engineered microorganism producing homosuccinic acid and method for preparing succinic acid using the same
MX2009006151A (es) Dispersiones de poliuretano de auto-entrelazamiento y libres de cosolventes.
WO2009157019A3 (fr) Préparation d'ezetimdie au moyen de nouveaux intermédiaires allyle
WO2010093182A3 (fr) Microorganisme permettant de produire des l-acides aminés et procédé de production de l-acides aminés l'utilisant
WO2010027150A3 (fr) Nouvelle préparation d’hydroxychloroquine
WO2009041473A1 (fr) Sel d'amine organique du 6-fluoro-3-hydroxy-2-pyrazinecarbonitrile et procédé de production
AU2016237099B2 (en) Method for producing novel nitrogen-containing compound or salt thereof, and production intermediate of same
ATE447593T1 (de) Niedrigviskose uretdiongruppenhaltige polyadditionsverbindungen, verfahren zur herstellung und verwendung
WO2010098583A2 (fr) Nouveau procédé de préparation de composés de statine ou des sels de ceux-ci, et composés intermédiaires utilisés dans ce procédé
EP2033960A3 (fr) Formule d'hydrate cristalline de linézolide et sels de linézolide
WO2008021491A3 (fr) Procédé de synthèse de 8-alkoxy-9h-isothiazolo[5,4-b]quinoline-3,4-diones
ATE486857T1 (de) Verfahren zur herstellung von telmisartan
WO2006024387A3 (fr) Biphenyl-thiazol-carboxamides
WO2006108792A8 (fr) Nouveaux derives heterocyclylethylbenzamide
ATE550944T1 (de) Pilzstämme und ein verfahren zur herstellung eines insektizids von diesen stämmen
UA96149C2 (en) Method for producing 4-oxoquinoline compound

Legal Events

Date Code Title Description
121 Ep: the epo has been informed by wipo that ep was designated in this application

Ref document number: 09833636

Country of ref document: EP

Kind code of ref document: A2

DPE1 Request for preliminary examination filed after expiration of 19th month from priority date (pct application filed from 20040101)
NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 09833636

Country of ref document: EP

Kind code of ref document: A2