WO2010141494A2 - Synthèse d'ézétimibe - Google Patents

Synthèse d'ézétimibe Download PDF

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Publication number
WO2010141494A2
WO2010141494A2 PCT/US2010/036938 US2010036938W WO2010141494A2 WO 2010141494 A2 WO2010141494 A2 WO 2010141494A2 US 2010036938 W US2010036938 W US 2010036938W WO 2010141494 A2 WO2010141494 A2 WO 2010141494A2
Authority
WO
WIPO (PCT)
Prior art keywords
formula
compound
alkyl
substituted
imine
Prior art date
Application number
PCT/US2010/036938
Other languages
English (en)
Other versions
WO2010141494A3 (fr
Inventor
Steven J. Collier
Jack Liang
Jasyln Fu Fan
Robert John Wilson
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

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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
    • 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 System
    • C07F5/02—Boron compounds
    • C07F5/025—Boronic and borinic acid compounds

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

Family

ID=43298448

Family Applications (1)

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

Country Status (1)

Country Link
WO (1) WO2010141494A2 (fr)

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012004382A1 (fr) * 2010-07-09 2012-01-12 Moehs Iberica S.L. Nouveau procédé de préparation d'ézétimibe
CN104402790A (zh) * 2014-12-28 2015-03-11 严白双 一种制备依折麦布的改进工艺
WO2015158191A1 (fr) * 2014-04-18 2015-10-22 上海方楠生物科技有限公司 Procédé pour la synthèse stéréosélective d'ézétimibe, médicament hypolipémiant
US9388440B2 (en) 2009-04-01 2016-07-12 Mylan Laboratories Limited 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
CN107677753A (zh) * 2017-11-24 2018-02-09 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, ISSN 0968-894X pages 311 - 314 *

Cited By (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US9388440B2 (en) 2009-04-01 2016-07-12 Mylan Laboratories Limited 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
WO2012004382A1 (fr) * 2010-07-09 2012-01-12 Moehs Iberica S.L. Nouveau procédé de préparation d'ézétimibe
WO2015158191A1 (fr) * 2014-04-18 2015-10-22 上海方楠生物科技有限公司 Procédé pour la synthèse stéréosélective d'ézétimibe, médicament hypolipémiant
CN104402790A (zh) * 2014-12-28 2015-03-11 严白双 一种制备依折麦布的改进工艺
CN104402790B (zh) * 2014-12-28 2016-09-28 严白双 一种制备依折麦布的改进工艺
CN107677753A (zh) * 2017-11-24 2018-02-09 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
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

Also Published As

Publication number Publication date
WO2010141494A3 (fr) 2011-04-21

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