EA201001352A1 - Промежуточные соединения для получения (3r,4s)-1-(4-фторфенил)-3-[(3s)-3-(4-фторфенил)-3-гидроксипропил]-4-(4-гидроксифенил)-2-ацетидинона - Google Patents
Промежуточные соединения для получения (3r,4s)-1-(4-фторфенил)-3-[(3s)-3-(4-фторфенил)-3-гидроксипропил]-4-(4-гидроксифенил)-2-ацетидинонаInfo
- Publication number
- EA201001352A1 EA201001352A1 EA201001352A EA201001352A EA201001352A1 EA 201001352 A1 EA201001352 A1 EA 201001352A1 EA 201001352 A EA201001352 A EA 201001352A EA 201001352 A EA201001352 A EA 201001352A EA 201001352 A1 EA201001352 A1 EA 201001352A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- fluoro
- phenyl
- propylene
- general formula
- obtaining
- Prior art date
Links
Classifications
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- 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
- C07D263/26—Oxygen atoms attached in position 2 with hetero atoms or acyl radicals directly attached to the ring nitrogen atom
-
- 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
-
- 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)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
Способ получения (S)-спиртооксазолидидов общей формулы II, где PG представляет собой водород или гидроксильную защитную группу, такую как триметилсилил, трет-бутилдиметилсилил, бензилокарбонил, трет-бутоксикарбонил, бензил, бензгидрил или тритил, в котором с кеталь оксазолидида общей формулы III, где PG имеет то же значение, что и выше, и R означает алкил с 1-4 атомами углерода, линейный или разветвленный, такой как метил, этил, изопропил или бутил, или R+R вместе представляют дивалентный алкил, или замещенный 1 или 2 алкильными группами, например, 1,2-этилен, 1,2-пропилен, 1,2-бутилен, 1,3-пропилен или 2,2-диметил-1,3-пропилен; снимают защиту действием кислотных реагентов в смеси воды и смешиваемого с водой растворителя в температурном диапазоне от 0 до 100°С (стадия А) и полученный кетон оксазолидид общей формулы IV, где PG имеет то же значение, что и выше, восстанавливают асимметричными реагентами в инертном органическом растворителе в температурном диапазоне от -30 до +40°С (стадия В).
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
CZ2008-107A CZ305066B6 (cs) | 2008-02-25 | 2008-02-25 | Způsob výroby (3R,4S)-1-(4-fluorfenyl)-3-[(3S)-3-(4-fluorfenyl)-3-hydroxypropyl)]-4-(4-hydroxyfenyl)-2-azetidinonu |
PCT/CZ2009/000016 WO2009106021A1 (en) | 2008-02-25 | 2009-02-13 | Intermediates for the preparation of (3r, 4s) -1- (4-fluorophenyl) -3- [ (3s) -3- (4-fluorophenyl) -3-hydroxypropyl) ] -4- (4-hydroxyphenyl) -2-azetidinone |
Publications (2)
Publication Number | Publication Date |
---|---|
EA201001352A1 true EA201001352A1 (ru) | 2011-02-28 |
EA017362B1 EA017362B1 (ru) | 2012-11-30 |
Family
ID=40599664
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA201001352A EA017362B1 (ru) | 2008-02-25 | 2009-02-13 | Промежуточные соединения для получения (3r,4s)-1-(4-фторфенил)-3-[(3s)-3-(4-фторфенил)-3-гидроксипропил]-4-(4-гидроксифенил)-2-азетидинона |
Country Status (6)
Country | Link |
---|---|
US (1) | US20110046389A1 (ru) |
EP (1) | EP2276753A1 (ru) |
CZ (1) | CZ305066B6 (ru) |
EA (1) | EA017362B1 (ru) |
UA (1) | UA103020C2 (ru) |
WO (1) | WO2009106021A1 (ru) |
Families Citing this family (9)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
HUP0501164A2 (en) * | 2005-12-20 | 2007-07-30 | Richter Gedeon Nyrt | New industrial process for the production of ezetimibe |
ATE445596T1 (de) * | 2005-12-22 | 2009-10-15 | Medichem Sa | Verfahren zur herstellung von zwischenprodukten für die herstellung von ezetimibe |
AR060216A1 (es) * | 2006-03-29 | 2008-06-04 | Medichem Sa | Procesos para preparar ezetimibe y compuestos intermediarios utiles para su preparacion |
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 |
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 |
CN102850390B (zh) * | 2011-07-01 | 2017-02-08 | 江苏豪森药业集团有限公司 | 依折麦布的中间体及其制备方法 |
CN103159751A (zh) * | 2011-12-13 | 2013-06-19 | 重庆华邦胜凯制药有限公司 | 苯酮酸酰胺缩酮衍生物的制备方法 |
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 |
EP3672939A1 (en) | 2017-08-21 | 2020-07-01 | Celgene Corporation | Processes for preparation of (s)-tert-butyl 4,5-diamino-5-oxopentanoate |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5631365A (en) * | 1993-09-21 | 1997-05-20 | Schering Corporation | Hydroxy-substituted azetidinone compounds useful as hypocholesterolemic agents |
US5739321A (en) * | 1996-05-31 | 1998-04-14 | Schering Corporation | 3-hydroxy γ-lactone based enantionselective synthesis of azetidinones |
US5886171A (en) * | 1996-05-31 | 1999-03-23 | Schering Corporation | 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones |
WO2000034240A1 (en) * | 1998-12-07 | 2000-06-15 | Schering Corporation | Process for the synthesis of azetidinones |
EP1851197A2 (en) * | 2005-02-09 | 2007-11-07 | Microbia, Inc. | Phenylazetidinone derivatives |
ATE445596T1 (de) * | 2005-12-22 | 2009-10-15 | Medichem Sa | Verfahren zur herstellung von zwischenprodukten für die herstellung von ezetimibe |
US20080032964A1 (en) * | 2006-04-10 | 2008-02-07 | Kansal Vinod K | Process for the synthesis of azetidinone |
-
2008
- 2008-02-25 CZ CZ2008-107A patent/CZ305066B6/cs not_active IP Right Cessation
-
2009
- 2009-02-13 EA EA201001352A patent/EA017362B1/ru not_active IP Right Cessation
- 2009-02-13 WO PCT/CZ2009/000016 patent/WO2009106021A1/en active Application Filing
- 2009-02-13 EP EP09714452A patent/EP2276753A1/en not_active Withdrawn
- 2009-02-13 US US12/918,869 patent/US20110046389A1/en not_active Abandoned
- 2009-02-13 UA UAA201011408A patent/UA103020C2/ru unknown
Also Published As
Publication number | Publication date |
---|---|
US20110046389A1 (en) | 2011-02-24 |
UA103020C2 (ru) | 2013-09-10 |
EA017362B1 (ru) | 2012-11-30 |
EP2276753A1 (en) | 2011-01-26 |
CZ2008107A3 (cs) | 2010-02-24 |
WO2009106021A1 (en) | 2009-09-03 |
CZ305066B6 (cs) | 2015-04-22 |
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Legal Events
Date | Code | Title | Description |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): AM AZ KG MD TJ TM |
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MM4A | Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s) |
Designated state(s): BY KZ |