WO2010071358A3 - Method of preparing ezetimibe and intermediates used therein - Google Patents
Method of preparing ezetimibe and intermediates used therein Download PDFInfo
- Publication number
- WO2010071358A3 WO2010071358A3 PCT/KR2009/007535 KR2009007535W WO2010071358A3 WO 2010071358 A3 WO2010071358 A3 WO 2010071358A3 KR 2009007535 W KR2009007535 W KR 2009007535W WO 2010071358 A3 WO2010071358 A3 WO 2010071358A3
- Authority
- WO
- WIPO (PCT)
- Prior art keywords
- intermediates used
- ezetimibe
- preparing ezetimibe
- preparing
- preventing
- Prior art date
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
- A61P3/06—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
- A61P9/10—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
- 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
Abstract
Disclosed is a method for preparing ezetimibe which is effective for preventing or treating arteriosclerosis, and novel intermediates used therein. In accordance with the method which does not use expensive reagents, unwanted diastereoisomers can be easily removed by a step-by-step crystallization procedure, and the ezetimibe of formula 1 can be prepared in a high yield without the use of a hydrogenation procedure under a high pressure.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
KR10-2008-0128457 | 2008-12-17 | ||
KR20080128457 | 2008-12-17 |
Publications (2)
Publication Number | Publication Date |
---|---|
WO2010071358A2 WO2010071358A2 (en) | 2010-06-24 |
WO2010071358A3 true WO2010071358A3 (en) | 2010-09-10 |
Family
ID=42269242
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PCT/KR2009/007535 WO2010071358A2 (en) | 2008-12-17 | 2009-12-16 | Method of preparing ezetimibe and intermediates used therein |
Country Status (4)
Country | Link |
---|---|
KR (1) | KR101156588B1 (en) |
AR (1) | AR074752A1 (en) |
TW (1) | TW201028374A (en) |
WO (1) | WO2010071358A2 (en) |
Families Citing this family (9)
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 |
WO2012076030A1 (en) | 2010-12-10 | 2012-06-14 | Pharmathen S.A. | Process for the preparation of intermediate compounds useful in the preparation of ezetimibe |
CN103086938A (en) * | 2011-10-28 | 2013-05-08 | 沈阳药科大学 | Ezetimibe synthesis method |
CN103204795B (en) * | 2012-01-11 | 2016-12-14 | 重庆华邦胜凯制药有限公司 | A kind of preparation method of chirality azetidinones |
CN103373970A (en) * | 2012-04-16 | 2013-10-30 | 重庆圣华曦药业股份有限公司 | Synthetic method for Ezetimibe intermediate |
CN106831522B (en) * | 2015-12-03 | 2021-06-08 | 中国科学院上海有机化学研究所 | Lactam compound and preparation method thereof |
CN106967106B (en) * | 2017-04-24 | 2018-08-10 | 上海华源医药科技发展有限公司 | A kind of production method of Ezetimibe intermediate |
KR102078158B1 (en) | 2018-02-21 | 2020-02-17 | 강원대학교산학협력단 | Process for preparing Ezetimibe and intermediate thereof |
US11110444B2 (en) | 2019-12-30 | 2021-09-07 | Industrial Technology Research Institute | Chiral catalyst and heterogeneous chiral catalyst comprising the same |
Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5886171A (en) * | 1996-05-31 | 1999-03-23 | Schering Corporation | 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones |
US6207822B1 (en) * | 1998-12-07 | 2001-03-27 | Schering Corporation | Process for the synthesis of azetidinones |
WO2007072088A1 (en) * | 2005-12-20 | 2007-06-28 | Richter Gedeon Nyrt. | Process for the production of ezetimibe and intermediates used in this proces |
Family Cites Families (2)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
CA2353981C (en) * | 1998-12-07 | 2005-04-26 | Schering Corporation | Process for the synthesis of azetidinones |
KR20070063592A (en) * | 2005-09-08 | 2007-06-19 | 테바 파마슈티컬 인더스트리즈 리미티드 | 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 |
-
2009
- 2009-12-15 AR ARP090104870A patent/AR074752A1/en not_active Application Discontinuation
- 2009-12-16 KR KR1020090125646A patent/KR101156588B1/en active IP Right Grant
- 2009-12-16 WO PCT/KR2009/007535 patent/WO2010071358A2/en active Application Filing
- 2009-12-16 TW TW098143111A patent/TW201028374A/en unknown
Patent Citations (3)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5886171A (en) * | 1996-05-31 | 1999-03-23 | Schering Corporation | 3-hydroxy gamma-lactone based enantioselective synthesis of azetidinones |
US6207822B1 (en) * | 1998-12-07 | 2001-03-27 | Schering Corporation | Process for the synthesis of azetidinones |
WO2007072088A1 (en) * | 2005-12-20 | 2007-06-28 | Richter Gedeon Nyrt. | Process for the production of ezetimibe and intermediates used in this proces |
Also Published As
Publication number | Publication date |
---|---|
WO2010071358A2 (en) | 2010-06-24 |
KR101156588B1 (en) | 2012-06-20 |
AR074752A1 (en) | 2011-02-09 |
KR20100070305A (en) | 2010-06-25 |
TW201028374A (en) | 2010-08-01 |
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