CY1111307T1 - Μεθοδος παραγωγης εζετιμιβης και ενδιαμεσες ενωσεις που χρησιμοποιουνται στην μεθοδο αυτη - Google Patents

Μεθοδος παραγωγης εζετιμιβης και ενδιαμεσες ενωσεις που χρησιμοποιουνται στην μεθοδο αυτη

Info

Publication number
CY1111307T1
CY1111307T1 CY20101101193T CY101101193T CY1111307T1 CY 1111307 T1 CY1111307 T1 CY 1111307T1 CY 20101101193 T CY20101101193 T CY 20101101193T CY 101101193 T CY101101193 T CY 101101193T CY 1111307 T1 CY1111307 T1 CY 1111307T1
Authority
CY
Cyprus
Prior art keywords
silyl
production
effectiveness
compounds used
viii
Prior art date
Application number
CY20101101193T
Other languages
English (en)
Inventor
József Bódi
Jànos Éles
Katalin Szöke
Krisztina Vukics
Tamás Gáti
Krisztina Temesvári
Dorottya Kiss-Bartos
Original Assignee
Richter Gedeon Nyrt.
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 Richter Gedeon Nyrt. filed Critical Richter Gedeon Nyrt.
Publication of CY1111307T1 publication Critical patent/CY1111307T1/el

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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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D317/00—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms
    • C07D317/08—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3
    • C07D317/10—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings
    • C07D317/14—Heterocyclic compounds containing five-membered rings having two oxygen atoms as the only ring hetero atoms having the hetero atoms in positions 1 and 3 not condensed with other rings with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D317/30—Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic 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
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • 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
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • C07F7/1872—Preparation; Treatments not provided for in C07F7/20
    • C07F7/1892—Preparation; Treatments not provided for in C07F7/20 by reactions not provided for in C07F7/1876 - C07F7/1888

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Multi-Process Working Machines And Systems (AREA)
  • Management, Administration, Business Operations System, And Electronic Commerce (AREA)
  • General Factory Administration (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Cephalosporin Compounds (AREA)

Abstract

Αυτή η εφεύρεση παρέχει μια νέα, βιομηχανικώς εύκολα πραγματοποιήσιμη και οικονομική μέθοδο που περιλαμβάνει μόνο μερικά στάδια, και βασίζεται σε νέες ενδιάμεσες ενώσεις για την παραγωγή 1-(4-)-3(R)-[3(S)-(4-φθοροφαινυλο)-3-υδροξυπροπυλο]-4(S)-(4-υδροξυφαινυλο)-2-αζετιδινόνης (εζετιμίβης) σύμφωνα με το παρακάτω σχήμα αντιδράσεων: (I),(II),(III),(IV),(V),(VI),(VII),(VIII),(IX),(Χ),(XI) όπου οι ουσίες των γενικών Τύπων II, IV, VI, VIII, IX, Χ και XI είναι νέες, ο Τύπος III είναι μη απομονωμένη ενδιάμεση ένωση, τα R1, R2 και R3 αντιπροσωπεύονται από τις ενώσεις των Τύπων Va-Vd, τα (Va), (Vb), (Vc), (Vd) και R4 είναι σιλυλο, π.χ. tert-βουτυλο-διμεθυλο-σιλυλο, tert-βουτυλο-διφαινυλο-σιλυλομάδα.
CY20101101193T 2005-12-20 2010-12-27 Μεθοδος παραγωγης εζετιμιβης και ενδιαμεσες ενωσεις που χρησιμοποιουνται στην μεθοδο αυτη CY1111307T1 (el)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
HU0501164A HUP0501164A2 (en) 2005-12-20 2005-12-20 New industrial process for the production of ezetimibe
EP06831516A EP1963260B1 (en) 2005-12-20 2006-12-18 Process for the production of ezetimibe and intermediates used in this process

Publications (1)

Publication Number Publication Date
CY1111307T1 true CY1111307T1 (el) 2015-08-05

Family

ID=37492156

Family Applications (1)

Application Number Title Priority Date Filing Date
CY20101101193T CY1111307T1 (el) 2005-12-20 2010-12-27 Μεθοδος παραγωγης εζετιμιβης και ενδιαμεσες ενωσεις που χρησιμοποιουνται στην μεθοδο αυτη

Country Status (18)

Country Link
US (1) US8178665B2 (el)
EP (1) EP1963260B1 (el)
CN (1) CN101346349B (el)
AT (1) ATE486848T1 (el)
CA (1) CA2630737A1 (el)
CY (1) CY1111307T1 (el)
DE (1) DE602006018063D1 (el)
DK (1) DK1963260T3 (el)
EA (1) EA014331B1 (el)
ES (1) ES2354728T3 (el)
HK (1) HK1128156A1 (el)
HR (1) HRP20110013T1 (el)
HU (2) HU0501164D0 (el)
PL (1) PL1963260T3 (el)
PT (1) PT1963260E (el)
RS (1) RS51613B (el)
SI (1) SI1963260T1 (el)
WO (1) WO2007072088A1 (el)

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UY29607A1 (es) 2005-06-20 2007-01-31 Astrazeneca Ab Compuestos quimicos
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
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
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AR060623A1 (es) 2006-04-27 2008-07-02 Astrazeneca Ab Compuestos derivados de 2-azetidinona y un metodo de preparacion
KR20080053948A (ko) * 2006-08-29 2008-06-16 테바 파마슈티컬 인더스트리즈 리미티드 (3ｒ,4ｓ)-4-(4-히드록시-보호된-페닐)-1-(4-플루오로페닐)-3-[3-(4-플루오로페닐)-3-옥소프로필]아제티딘-2-온의정제 방법
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
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CN102477008B (zh) * 2010-11-22 2014-05-21 沈阳药科大学 依泽替米贝的合成方法
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CN102731489B (zh) * 2011-04-11 2016-10-26 天津药物研究院有限公司 一种依折麦布关键中间体的制备方法
CN102952055A (zh) * 2011-08-16 2013-03-06 凯瑞斯德生化(苏州)有限公司 一种依泽替米贝和其中间体的制备方法
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
CN103896700B (zh) * 2012-12-25 2015-12-23 浙江九洲药物科技有限公司 依泽替米贝手性中间体的制备方法
CN103450065B (zh) * 2013-07-15 2015-10-14 和鼎（南京）医药技术有限公司 制备依泽替米贝的方法
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
CN104892537B (zh) * 2015-05-15 2018-07-17 江西施美药业股份有限公司 依折麦布中间体以及依折麦布的合成方法
CN105566243B (zh) * 2016-01-15 2017-10-31 齐鲁天和惠世制药有限公司 从依折麦布生产废液中回收(s)‑(+)‑4‑苯基‑2‑噁唑烷酮的方法
CN107098841A (zh) * 2016-02-19 2017-08-29 常州方楠医药技术有限公司 一种依折麦布的制备方法及该方法中所用的中间体
CN107488138B (zh) * 2016-06-10 2021-05-04 山东新时代药业有限公司 一种依折麦布合成方法
CN107488164B (zh) * 2016-06-10 2020-08-14 山东新时代药业有限公司 一种依折麦布中间体化合物
CN107488165B (zh) * 2016-06-10 2021-05-04 山东新时代药业有限公司 一种依折麦布中间体化合物
CN107488173B (zh) * 2016-06-10 2021-05-04 山东新时代药业有限公司 一种依折麦布中间体及其合成方法
CN107488190B (zh) * 2016-06-10 2021-07-02 山东新时代药业有限公司 一种依折麦布中间体及其制备方法

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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
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CZ305066B6 (cs) * 2008-02-25 2015-04-22 Zentiva, K.S. Způsob 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

Also Published As

Publication number Publication date
EA014331B1 (ru) 2010-10-29
PL1963260T3 (pl) 2011-04-29
WO2007072088A1 (en) 2007-06-28
US20090216009A1 (en) 2009-08-27
CN101346349A (zh) 2009-01-14
HUP0501164A2 (en) 2007-07-30
SI1963260T1 (sl) 2011-02-28
EA200801548A1 (ru) 2008-10-30
RS51613B (en) 2011-08-31
CA2630737A1 (en) 2007-06-28
ATE486848T1 (de) 2010-11-15
HK1128156A1 (en) 2009-10-16
DK1963260T3 (da) 2011-01-17
HRP20110013T1 (hr) 2011-02-28
DE602006018063D1 (de) 2010-12-16
EP1963260A1 (en) 2008-09-03
HU0501164D0 (en) 2006-02-28
US8178665B2 (en) 2012-05-15
ES2354728T3 (es) 2011-03-17
EP1963260B1 (en) 2010-11-03
CN101346349B (zh) 2011-04-20
PT1963260E (pt) 2010-12-27

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