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BRPI0605934A2 - processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba - Google Patents

processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba

Info

Publication number
BRPI0605934A2
BRPI0605934A2 BRPI0605934-1A BRPI0605934A BRPI0605934A2 BR PI0605934 A2 BRPI0605934 A2 BR PI0605934A2 BR PI0605934 A BRPI0605934 A BR PI0605934A BR PI0605934 A2 BRPI0605934 A2 BR PI0605934A2
Authority
BR
Brazil
Prior art keywords
compound
fluorophenyl
processes
preparing
azetidinone
Prior art date
Application number
BRPI0605934-1A
Other languages
English (en)
Inventor
Vinod Kumar Kansal
Sunhail Ahmad
Bhupendra Tyagi
Nitin Gupta
Nurit Perlman
Original Assignee
Teva Pharma
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 Teva Pharma filed Critical Teva Pharma
Publication of BRPI0605934A2 publication Critical patent/BRPI0605934A2/pt

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
    • A61P3/04—Anorexiants; Antiobesity agents
    • 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
    • A61P9/12—Antihypertensives
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

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

Abstract

PROCESSOS PARA A PREPARAçãO DE (3R,4S)-4-((4-BENZILOXI)FENIL)-1-(4-FLUOROFENIL)-3-((S)-3-(4-F LUOROFENIL)-3-HIDROXIPROPIL)-2-AZETIDINONA, UM INTERMEDIáRIO PARA A SìNTESE DE EZETIMIBA. A invenção abrange (3R,4S)-4-((4-benziloxi)fenil)-1-(4-fluorofenil)-3-(4-fluorofenil)-3-oxopro pil)-2-azetidinona (Composto 2a) tendo uma pureza enanciomérica de pelo menos cerca de 97,5%. A invenção também abrange o Composto 2a tendo uma pureza química de pelo menos 97%. A invenção abrange adicionalmente processos para preparar o Composto 2a a partir do Composto 1 tendo a seguinte fórmula (1) . Composto 1. A invenção abrange também processos para preparar um composto tendo a fórmula (II), a partir de um composto tendo a seguinte fórmula (III), em que R é selecionado no grupo que consiste de: H ou um grupo protetor de hidroxil. A invenção também abrange processos para preparar o Composto 2a, preferivelmente para formar o Composto 2a-Eorma 01. Também inclui processos para preparar ezetimiba a partir do Composto 2a-Forma 01 ou Composto 2a preparado de acordo com a invenção, composições contendo a referida ezetimiba e métodos para reduzir o colesterol usando as referidas composições.
BRPI0605934-1A 2005-09-08 2006-09-08 processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba BRPI0605934A2 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US71591905P 2005-09-08 2005-09-08
US83243006P 2006-07-20 2006-07-20
PCT/US2006/035060 WO2007030721A2 (en) 2005-09-08 2006-09-08 Processes for the preparation of (3r,4s)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((s)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe

Publications (1)

Publication Number Publication Date
BRPI0605934A2 true BRPI0605934A2 (pt) 2009-05-26

Family

ID=37671943

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0605934-1A BRPI0605934A2 (pt) 2005-09-08 2006-09-08 processos para a preparação de ( 3r, 4s) - 4 - ( (4-benziloxi ) fenil ) - 1 - ( 4 - fluorofenil ) - 3 - ( (s) - 3 - ( 4 - fluorofenil ) - 3 - hidroxipropil) - 2 - azetidinona, um intermediário para a sìntese da ezetimiba

Country Status (9)

Country Link
US (2) US20070259845A1 (pt)
EP (1) EP1922304A2 (pt)
JP (1) JP2008517951A (pt)
KR (1) KR20070063592A (pt)
BR (1) BRPI0605934A2 (pt)
CA (1) CA2616058A1 (pt)
IL (1) IL186326A0 (pt)
MX (1) MX2007005493A (pt)
WO (1) WO2007030721A2 (pt)

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GB0215579D0 (en) 2002-07-05 2002-08-14 Astrazeneca Ab Chemical compounds
CN1870988A (zh) * 2003-10-30 2006-11-29 默克公司 作为抗高胆固醇血症药的2－氮杂环丁烷酮
WO2005061452A1 (en) 2003-12-23 2005-07-07 Astrazeneca Ab Diphenylazetidinone derivates possessing cholesterol absorption inhibitory activity
UY29607A1 (es) 2005-06-20 2007-01-31 Astrazeneca Ab Compuestos quimicos
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
AR057072A1 (es) 2005-06-22 2007-11-14 Astrazeneca Ab Compuestos quimicos derivados de 2-azetidinona, formulacion farmaceutica y un proceso de preparacion del compuesto
HU0501164D0 (en) * 2005-12-20 2006-02-28 Richter Gedeon Vegyeszet New industrial process for the production of ezetimibe
WO2007119106A2 (en) * 2005-12-22 2007-10-25 Medichem, S.A. Processes for preparing intermediate compounds useful for the preparation 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
CA2644905A1 (en) * 2006-03-06 2007-09-13 Teva Pharmaceutical Industries Ltd. Ezetimibe compositions
WO2007144780A2 (en) * 2006-03-29 2007-12-21 Medichem S.A. Processes for preparing ezetimibe and intermediate compounds useful for the preparation thereof
AR060623A1 (es) 2006-04-27 2008-07-02 Astrazeneca Ab Compuestos derivados de 2-azetidinona y un metodo de preparacion
WO2008032338A2 (en) * 2006-09-11 2008-03-20 Manne Satyanarayana Reddy Improved process for the preparation of ezetimibe and its intermediates
CN101679236B (zh) * 2007-01-24 2013-03-06 克尔克公司 依泽替米贝的制备方法和其的衍生物
EP1953140A1 (en) * 2007-01-24 2008-08-06 Krka Process for the preparation of ezetimibe and derivatives thereof
US20090047716A1 (en) * 2007-06-07 2009-02-19 Nurit Perlman Reduction processes for the preparation of ezetimibe
EP2155667A1 (en) * 2007-06-07 2010-02-24 Teva Pharmaceutical Industries Ltd. Reduction processes for the preparation of ezetimibe
WO2009032264A1 (en) * 2007-08-30 2009-03-12 Teva Pharmaceutical Industries Ltd. Processes for preparing intermediates of ezetimibe by microbial reduction
US8013189B2 (en) * 2007-09-21 2011-09-06 Basf Se Accelerated amide and ester reductions with amine boranes and additives
CZ2007843A3 (cs) * 2007-11-30 2009-06-10 Zentiva, A. S. Zpusob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu a jeho meziprodukty
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
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WO2010113175A2 (en) 2009-04-01 2010-10-07 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
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WO2014019166A1 (zh) * 2012-08-01 2014-02-06 上海威智医药科技有限公司 高活性硼烷类化合物的工业化生产方法
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JP6795974B2 (ja) * 2014-03-06 2020-12-02 日産化学株式会社 光学活性アゼチジノン化合物の製造方法
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Also Published As

Publication number Publication date
KR20070063592A (ko) 2007-06-19
IL186326A0 (en) 2008-01-20
US20070259845A1 (en) 2007-11-08
WO2007030721A3 (en) 2007-05-31
MX2007005493A (es) 2007-09-11
EP1922304A2 (en) 2008-05-21
JP2008517951A (ja) 2008-05-29
WO2007030721A2 (en) 2007-03-15
US20100010212A1 (en) 2010-01-14
CA2616058A1 (en) 2007-03-15
WO2007030721A9 (en) 2008-04-24

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Legal Events

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B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE AS 4A E 5A ANUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2161 DE 05/06/2012.