WO2003004457A3 - Preparation process for atorvastatin and intermediates - Google Patents

Preparation process for atorvastatin and intermediates Download PDF

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Publication number
WO2003004457A3
WO2003004457A3 PCT/EP2002/007014 EP0207014W WO03004457A3 WO 2003004457 A3 WO2003004457 A3 WO 2003004457A3 EP 0207014 W EP0207014 W EP 0207014W WO 03004457 A3 WO03004457 A3 WO 03004457A3
Authority
WO
WIPO (PCT)
Prior art keywords
oxo
intermediates
atorvastatin
preparation process
phenylethyl
Prior art date
Application number
PCT/EP2002/007014
Other languages
French (fr)
Other versions
WO2003004457A2 (en
Inventor
Kai-Uwe Schoening
Jemima Hartwig
Original Assignee
Ciba Sc Holding Ag
Kai-Uwe Schoening
Jemima Hartwig
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 Ciba Sc Holding Ag, Kai-Uwe Schoening, Jemima Hartwig filed Critical Ciba Sc Holding Ag
Priority to AU2002325845A priority Critical patent/AU2002325845A1/en
Publication of WO2003004457A2 publication Critical patent/WO2003004457A2/en
Publication of WO2003004457A3 publication Critical patent/WO2003004457A3/en

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Classifications

    • 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
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C231/00—Preparation of carboxylic acid amides
    • C07C231/12—Preparation of carboxylic acid amides by reactions not involving the formation of carboxamide groups
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic 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
    • C07D207/30—Heterocyclic 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
    • C07D207/34—Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

The invention relates to a novel process for the preparation of 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide and to novel intermediates and process steps therefor. In that process inter alia the intermediate 2-[2-(4-fluorophenyl)-2-oxo-1-phenylethyl]-4-methyl-3-oxo-pentanoic acid phenylamide is obtained by nucleophilic substitution from a compound of formula (I), wherein X is a nucleofugal leaving group, with a ketoamide of formula (II) in the presence of a base.
PCT/EP2002/007014 2001-07-04 2002-06-25 Preparation process for atorvastatin and intermediates WO2003004457A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002325845A AU2002325845A1 (en) 2001-07-04 2002-06-25 Preparation process for atorvastatin and intermediates

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP01810651.8 2001-07-04
EP01810651 2001-07-04

Publications (2)

Publication Number Publication Date
WO2003004457A2 WO2003004457A2 (en) 2003-01-16
WO2003004457A3 true WO2003004457A3 (en) 2003-03-20

Family

ID=8184003

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2002/007014 WO2003004457A2 (en) 2001-07-04 2002-06-25 Preparation process for atorvastatin and intermediates

Country Status (2)

Country Link
AU (1) AU2002325845A1 (en)
WO (1) WO2003004457A2 (en)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004108660A1 (en) 2003-06-09 2004-12-16 Biocon Limited Novel halo-substituted active methylene compounds
WO2004103957A1 (en) * 2003-05-22 2004-12-02 Biocon Limited Novel dithioketal
JP2008510797A (en) * 2004-08-26 2008-04-10 バイオコン・リミテッド Process for producing 4-fluoro-α- [2-methyl-1-oxopropyl] γ-oxo-N-β-diphenylbenzenebutanamide
EP1671947A1 (en) * 2004-12-20 2006-06-21 Ratiopharm GmbH Process for preparing pyrrole derivatives and intermediates
KR100665794B1 (en) 2004-12-31 2007-01-09 주식회사유한양행 A novel process for preparing 4-4-fluorophenyl-2-isobutiryl-3-phenyl-4-oxo-n-phenyl-butylamide
CN101306988B (en) * 2007-05-15 2011-11-30 浙江京新药业股份有限公司 New method for synthesizing alpha-brom-4-fluoro phenylpropiophenone
WO2009144736A1 (en) * 2008-05-29 2009-12-03 Arch Pharmalabs Limited NOVEL PROCESS FOR THE PREPARATION OF 4-FLUORO-ALPHA-[2-METHYL -1-OXOPROPYL]-GAMMA-OXO-N-ß-DIPHENYLBENZENEBUTANAMIDE AND PRODUCTS THEREFROM
WO2012143933A1 (en) * 2011-04-21 2012-10-26 Vijayasri Organics Limited A PROCESS FOR PREPARATION OF 4-FLUORO-α-[2-METHYL-L-OXOPROPYL]-γ-OXO-N-β-DIPHENYLBENZENE BUTANE AMIDE
CN102617440B (en) * 2012-03-07 2013-11-06 湖南欧亚生物有限公司 Method for preparing atorvastatin calcium
CN106588689A (en) * 2016-12-15 2017-04-26 河南豫辰药业股份有限公司 Method for recycling atorvastatin intermediate M4 from crystallization mother liquor waste liquor
CN114195670B (en) * 2021-12-31 2024-03-15 河南豫辰药业股份有限公司 Refining method of atorvastatin mother nucleus M4

Citations (1)

* 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

Patent Citations (1)

* 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

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
BAUMANN K L ET AL: "THE CONVERGENT SYNTHESIS OF CI-981, AN OPTICALLY ACTIVE, HIGHLY POTENT, TISSUE SELECTIVE INHIBITOR OF HMG-COA REDUCTASE", TETRAHEDRON LETTERS, ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, NL, vol. 33, no. 17, 21 April 1992 (1992-04-21), pages 2283 - 2284, XP000608147, ISSN: 0040-4039 *
GRAUL A ET AL: "ATORVASTATIN CALCIUM", DRUGS OF THE FUTURE, BARCELONA, ES, vol. 22, no. 9, 1997, pages 956 - 968, XP000904817, ISSN: 0377-8282 *

Also Published As

Publication number Publication date
AU2002325845A1 (en) 2003-01-21
WO2003004457A2 (en) 2003-01-16

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