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WO2009054693A3 - Process for the preparation of atorvastatin - Google Patents

Process for the preparation of atorvastatin Download PDF

Info

Publication number
WO2009054693A3
WO2009054693A3 PCT/KR2008/006290 KR2008006290W WO2009054693A3 WO 2009054693 A3 WO2009054693 A3 WO 2009054693A3 KR 2008006290 W KR2008006290 W KR 2008006290W WO 2009054693 A3 WO2009054693 A3 WO 2009054693A3
Authority
WO
WIPO (PCT)
Prior art keywords
atorvastatin
preparing
preparation
compound
phenylcarbamoyl
Prior art date
Legal status (The legal status 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 status listed.)
Ceased
Application number
PCT/KR2008/006290
Other languages
French (fr)
Other versions
WO2009054693A2 (en
Inventor
Young Mook Lim
Young Taek Han
Byung Goo Lee
Yoon Seok Song
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Daewoong Pharmaceutical Co Ltd
Daewoong Bio Inc
Original Assignee
Daewoong Pharmaceutical Co Ltd
Daewoong Bio 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 Daewoong Pharmaceutical Co Ltd, Daewoong Bio Inc filed Critical Daewoong Pharmaceutical Co Ltd
Publication of WO2009054693A2 publication Critical patent/WO2009054693A2/en
Publication of WO2009054693A3 publication Critical patent/WO2009054693A3/en
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/30Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
    • C07D207/34Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00Drugs for disorders of the metabolism
    • A61P3/06Antihyperlipidemics
    • YGENERAL 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
    • Y02TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02PCLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00Technologies relating to chemical industry
    • Y02P20/50Improvements relating to the production of bulk chemicals
    • Y02P20/55Design 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)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pyrrole Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

The present invention relates to a process for preparing the cholesterol biosynthesis inhibitor atorvastatin, (3R,5R)-7-[2-(4-fluorophenyl)-5-isopropyl-3-phenyl-4- (phenylcarbamoyl)-lH-pyrrol-l-yl]-3,5-dihydroxyheptanoic acid calcium salt, which comprises a step of preparing a beta-keto ester compound using a diazoacetate compound.
PCT/KR2008/006290 2007-10-25 2008-10-24 Process for the preparation of atorvastatin Ceased WO2009054693A2 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
KR1020070108007A KR100921195B1 (en) 2007-10-25 2007-10-25 How to prepare atorvastatin
KR10-2007-0108007 2007-10-25

Publications (2)

Publication Number Publication Date
WO2009054693A2 WO2009054693A2 (en) 2009-04-30
WO2009054693A3 true WO2009054693A3 (en) 2009-06-18

Family

ID=40580255

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/KR2008/006290 Ceased WO2009054693A2 (en) 2007-10-25 2008-10-24 Process for the preparation of atorvastatin

Country Status (3)

Country Link
KR (1) KR100921195B1 (en)
TW (1) TW200925149A (en)
WO (1) WO2009054693A2 (en)

Families Citing this family (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN110372677B (en) * 2019-07-25 2021-01-05 浙江海森药业股份有限公司 Method for preparing atorvastatin key intermediate L1 by solvent-free method
CN114539119A (en) * 2020-11-26 2022-05-27 广东东阳光药业有限公司 A kind of preparation method of atorvastatin

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989007598A2 (en) * 1988-02-22 1989-08-24 Warner-Lambert Company Improved process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5273995A (en) * 1989-07-21 1993-12-28 Warner-Lambert Company [R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl-3-phenyl-4-[(phenylamino) carbonyl]- 1H-pyrrole-1-heptanoic acid, its lactone form and salts thereof
KR20060007924A (en) * 2004-07-23 2006-01-26 한국화학연구원 Method for preparing 2- [6- (aminoalkyl) -1,3-dioxan-4-yl] acetic acid derivative having optical activity

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1989007598A2 (en) * 1988-02-22 1989-08-24 Warner-Lambert Company Improved process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis
US5273995A (en) * 1989-07-21 1993-12-28 Warner-Lambert Company [R-(R*R*)]-2-(4-fluorophenyl)-β,δ-dihydroxy-5-(1-methylethyl-3-phenyl-4-[(phenylamino) carbonyl]- 1H-pyrrole-1-heptanoic acid, its lactone form and salts thereof
KR20060007924A (en) * 2004-07-23 2006-01-26 한국화학연구원 Method for preparing 2- [6- (aminoalkyl) -1,3-dioxan-4-yl] acetic acid derivative having optical activity

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
BLACK, A. E. ET AL.: "Metabolism and excretion of atorvastatin in rats and dogs.", DRUG METABOLISM AND DISPOSITION., vol. 27, no. 8, 1999, pages 916 - 923 *

Also Published As

Publication number Publication date
KR100921195B1 (en) 2009-10-13
TW200925149A (en) 2009-06-16
WO2009054693A2 (en) 2009-04-30
KR20090042097A (en) 2009-04-29

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