WO2010141494A3 - Synthèse d'ézétimibe - Google Patents

Synthèse d'ézétimibe Download PDF

Info

Publication number
WO2010141494A3
WO2010141494A3 PCT/US2010/036938 US2010036938W WO2010141494A3 WO 2010141494 A3 WO2010141494 A3 WO 2010141494A3 US 2010036938 W US2010036938 W US 2010036938W WO 2010141494 A3 WO2010141494 A3 WO 2010141494A3
Authority
WO
WIPO (PCT)
Prior art keywords
ezetimibe
synthesis
fluorophenyl
azetidinone
hydroxyphenyl
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/US2010/036938
Other languages
English (en)
Other versions
WO2010141494A2 (fr
Inventor
Steven J. Collier
Jack Liang
Jasyln Fu Fan
Robert John Wilson
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.)
Codexis Inc
Original Assignee
Codexis Inc
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 Codexis Inc filed Critical Codexis Inc
Publication of WO2010141494A2 publication Critical patent/WO2010141494A2/fr
Publication of WO2010141494A3 publication Critical patent/WO2010141494A3/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
    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C251/00—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton
    • C07C251/02—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups
    • C07C251/24—Compounds containing nitrogen atoms doubly-bound to a carbon skeleton containing imino groups having carbon atoms of imino groups bound to carbon atoms of six-membered aromatic rings
    • 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
    • C07D263/24—Oxygen atoms attached in position 2 with hydrocarbon radicals, substituted by oxygen atoms, attached to other ring carbon atoms
    • 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
    • C07F5/00—Compounds containing elements of Groups 3 or 13 of the Periodic Table
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Urology & Nephrology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (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)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La présente invention concerne des procédés de préparation d'ézétimibe (1-(4-fluorophényl)-3(R)-[3-(4-fluorophényl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphényl)-2-azétidinone) et de composés d'azétidine apparentés.
PCT/US2010/036938 2009-06-02 2010-06-01 Synthèse d'ézétimibe Ceased WO2010141494A2 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US18307709P 2009-06-02 2009-06-02
US61/183,077 2009-06-02

Publications (2)

Publication Number Publication Date
WO2010141494A2 WO2010141494A2 (fr) 2010-12-09
WO2010141494A3 true WO2010141494A3 (fr) 2011-04-21

Family

ID=43298448

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/US2010/036938 Ceased WO2010141494A2 (fr) 2009-06-02 2010-06-01 Synthèse d'ézétimibe

Country Status (1)

Country Link
WO (1) WO2010141494A2 (fr)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2010113175A2 (fr) 2009-04-01 2010-10-07 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
ES2372460B1 (es) * 2010-07-09 2012-11-16 Moehs Ibérica S.L. Nuevo método para la preparación de ezetimiba.
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
CN104402790B (zh) * 2014-12-28 2016-09-28 严白双 一种制备依折麦布的改进工艺
CN107677753B (zh) * 2017-11-24 2021-03-16 中山奕安泰医药科技有限公司 一种依替米贝中间体的检测方法

Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000034240A1 (fr) * 1998-12-07 2000-06-15 Schering Corporation Procede relatif a la synthese d'azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
US20060135755A1 (en) * 2004-12-20 2006-06-22 Schering Corporation Process for the synthesis of azetidinones
WO2007017705A1 (fr) * 2005-08-09 2007-02-15 Glenmark Pharmaceuticals Limited Procede de preparation d'azetidinones

Patent Citations (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2000034240A1 (fr) * 1998-12-07 2000-06-15 Schering Corporation Procede relatif a la synthese d'azetidinones
US6207822B1 (en) * 1998-12-07 2001-03-27 Schering Corporation Process for the synthesis of azetidinones
US20060135755A1 (en) * 2004-12-20 2006-06-22 Schering Corporation Process for the synthesis of azetidinones
WO2007017705A1 (fr) * 2005-08-09 2007-02-15 Glenmark Pharmaceuticals Limited Procede de preparation d'azetidinones

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
DUANE A. BURNETT ET AL.: "Synthesis of iodinated biochemical tools related to the 2-azetidinone class of cholesterol absorption inhibitors", BIOORGANIC & MEDICINAL CHEMISTRY LETTERS, vol. 2, no. 3, 2002, pages 311 - 314, XP002275928, DOI: doi:10.1016/S0960-894X(01)00750-8 *

Also Published As

Publication number Publication date
WO2010141494A2 (fr) 2010-12-09

Similar Documents

Publication Publication Date Title
WO2007120824A3 (fr) Procédés de synthèse de l'azétidinone
IL186326A0 (en) Processes for the preparation of (3r,4s)-4-((4-benzyloxyl)phenyl)-1-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe
NO20080416L (no) Forbedrede prosesser for fremstilling av Ezetimibe
WO2007119106A3 (fr) Procédés de préparation de composés intermédiaires utilisés dans la préparation de l'ézétimibe
EP2288610B8 (fr) Dérivés d'azétidine et de cyclobutane en tant qu'inhibiteurs de janus kinase (jak)
WO2010141494A3 (fr) Synthèse d'ézétimibe
ZA200705130B (en) Process for the synthesis of azetidinones
GB2490435B (en) Synthesis of diester-based lubricants from enzymatically-directed epoxides
MY156954A (en) PROCESS FOR PREPARING SUBSTITUTED 1-O-ACYL-2-DEOXY-2-FLUORO-4-THIO-ß-D-ARABINOFURANOSES
ZA200710609B (en) Novel 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
IL185419A0 (en) Improved process for the synthesis of enantiomeric indanylamine derivatives
IL187741A0 (en) Novel 2-azetidinone derivatives as cholesterol absorption inhibitors for the treatment of hyperlipidaemic conditions
EP2006290A4 (fr) Procédé amélioré de production d'un composé de carbapenem
WO2009067960A3 (fr) Procédé de fabrication de (3r,4s)-l-(4-fluorophényl)-3-[(3s)-3-(4-fluorophényl)-3-hydroxypropyl)]-4-(4-hydroxyphényl)-2-azétidinone et ses intermédiaires
WO2009092702A3 (fr) Carboxylate de ((2s,4r)-4,6-dihydroxytétrahydro-2h-pyran-2-yl)méthyle et son procédé de fabrication
WO2009005647A3 (fr) Composés et procédé de préparation d'intermédiaires chiraux pour la synthèse de la proxétine
WO2008032338A3 (fr) Procédé amélioré de préparation d'ézétimibe et de ses intermédiaires
WO2009140932A3 (fr) Procédé de production de (3r,4s)-l-(4-fluorophényl)-3-[(3s)-3-(4-fluorophényl)- hydroxypropyl)] -4-(4-hydroxyphényl) -2-azétidinone
PL2326325T3 (pl) Pochodna azetydyny do leczenia neuropatii obwodowych
WO2012116349A3 (fr) Nouveaux cocristaux d'ézétimibe
EP2566497A4 (fr) Biocatalyseurs pour la synthèse d'ézétimibe
WO2012173504A3 (fr) Procédé de synthèse d'azétidinones substituées et intermédiaires à cet effet
TR201000116A1 (tr) (3r,4s)-l-(4-florofenil)-3-[(3s)-3-(4-florofenil)-3-hidroks propil-4-(4-hidroksifenil)azetidin-2-on hazırlanması için uygun yeni ara ürünler ve bunların üretimi için prosesler.
ZA200902732B (en) Method for the synthesis of n-[3-(2-methoxyphenyl)sulfanyl]-2-methoylpropyl]-3,4-dihydro-2h-1,5-benzoxathiepin-3-amine
WO2010105267A3 (fr) Composés de β-lactame

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: 10783944

Country of ref document: EP

Kind code of ref document: A2

NENP Non-entry into the national phase

Ref country code: DE

122 Ep: pct application non-entry in european phase

Ref document number: 10783944

Country of ref document: EP

Kind code of ref document: A2