CO5601005A2 - Proceso para la elaboracion de inhibidores de reductasa hmg-coa - Google Patents

Proceso para la elaboracion de inhibidores de reductasa hmg-coa

Info

Publication number
CO5601005A2
CO5601005A2 CO04077715A CO04077715A CO5601005A2 CO 5601005 A2 CO5601005 A2 CO 5601005A2 CO 04077715 A CO04077715 A CO 04077715A CO 04077715 A CO04077715 A CO 04077715A CO 5601005 A2 CO5601005 A2 CO 5601005A2
Authority
CO
Colombia
Prior art keywords
hmg
elaboration
coa reductase
reductase inhibitors
sub
Prior art date
Application number
CO04077715A
Other languages
English (en)
Inventor
Murat Acemoglu
Bernhard Riss
Original Assignee
Novartis Ag
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 Novartis Ag filed Critical Novartis Ag
Publication of CO5601005A2 publication Critical patent/CO5601005A2/es

Links

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
    • 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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • C07D209/00—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D209/02—Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom condensed with one carbocyclic ring
    • C07D209/04—Indoles; Hydrogenated indoles
    • C07D209/10—Indoles; Hydrogenated indoles with substituted hydrocarbon radicals attached to carbon atoms of the hetero ring
    • C07D209/18—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
    • C07D215/00—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
    • C07D215/02—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
    • C07D215/12—Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
    • C07D215/14—Radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
    • C07B2200/00—Indexing scheme relating to specific properties of organic compounds
    • C07B2200/07—Optical isomers

Landscapes

  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Urology & Nephrology (AREA)
  • Obesity (AREA)
  • Diabetes (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Quinoline Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Indole Compounds (AREA)
  • Enzymes And Modification Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

1.- Un proceso para la elaboración de una forma enantioméricamente pura o una forma racémica de un compuesto de la fórmula o una sal, especialmente una sal farmacéuticamente aceptable con una base, del mismo o una lactona del mismo, en donde el elemento - - - - - - representa -CH2CH2- o -CH=CH- y R representa un residuo cíclico; comprendiendo (a) reaccionar los compuestos (llla) o (IIIb) en donde X4 y X5, independientemente de otro, representa alquilo C1-C7 o fenil-C1-C7-alquilo; X6, X7 y X8, independientemente de otro, representa fenilo que se sustituye o no se sustituye por uno o más sustituyentes seleccionados el grupo que consiste de alquilo C1-C7, hidroxi, alcoxi C1-C7, alcanoil-oxi C2-C8, halógeno, nitro, ciano y CF3; y Hal¯ representa un anión de haluro; con un alcano metalizado para formar el iluro y después el intermedio de iluro resultante con un compuesto de la fórmula en donde X representa hidroxi eterificado, hidroxi esterificado, o amino mono- o di-sustituido; X1 es hidroxi protegido; X2 representa alquilo C1-C7; y X3 representa hidrógeno o uno o más sustituyentes, por ejemplo, seleccionados del grupo que consiste de alquilo C1-C7, alcanoil-oxi C2-C8, halógeno, nitro, ciano, y CF3; (b) opcionalmente, si se desea, convertir un compuesto resultante de la fórmula (III d) en donde X1, X2 y X3 tienen los significados según se definen anteriormente y Y representa un grupo de la fórmula (X4O)(X5O)P(=O)- o (X6)(X7)(X8)P+ Hal¯ y ....
CO04077715A 2002-01-31 2004-08-10 Proceso para la elaboracion de inhibidores de reductasa hmg-coa CO5601005A2 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US35378702P 2002-01-31 2002-01-31

Publications (1)

Publication Number Publication Date
CO5601005A2 true CO5601005A2 (es) 2006-01-31

Family

ID=27663254

Family Applications (1)

Application Number Title Priority Date Filing Date
CO04077715A CO5601005A2 (es) 2002-01-31 2004-08-10 Proceso para la elaboracion de inhibidores de reductasa hmg-coa

Country Status (23)

Country Link
US (2) US7371865B2 (es)
EP (1) EP1472228B1 (es)
JP (1) JP4524111B2 (es)
KR (1) KR20040081161A (es)
CN (1) CN1305853C (es)
AT (1) ATE426594T1 (es)
AU (1) AU2003226971B2 (es)
BR (1) BR0307303A (es)
CA (1) CA2472776C (es)
CO (1) CO5601005A2 (es)
DE (1) DE60326819D1 (es)
EC (1) ECSP045214A (es)
ES (1) ES2323267T3 (es)
HK (1) HK1070651A1 (es)
IL (1) IL162980A (es)
MX (1) MXPA04007396A (es)
NO (1) NO327091B1 (es)
NZ (1) NZ534232A (es)
PL (1) PL370658A1 (es)
PT (1) PT1472228E (es)
RU (1) RU2299196C2 (es)
WO (1) WO2003064392A1 (es)
ZA (1) ZA200405322B (es)

Families Citing this family (22)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2004072040A1 (en) * 2003-02-12 2004-08-26 Ciba Specialty Chemicals Holding Inc. Crystalline forms of pitavastatin calcium
CN100408562C (zh) * 2003-04-24 2008-08-06 大赛璐化学工业株式会社 (3r,5s,6e)-7-[2-环丙基-4-(4-氟苯基)喹啉-3-基]-3,5-二羟基-6-庚烯酸乙酯的制备方法
TWI328006B (en) * 2003-12-26 2010-08-01 Nissan Chemical Ind Ltd Crystal form of quinoline compound and process for its production
EP1817027A2 (en) * 2004-09-27 2007-08-15 Ranbaxy Laboratories Limited Process for preparating enantiomerically pure fluvastatin sodium and a novel polymorphic form thereof
US8455640B2 (en) * 2006-05-03 2013-06-04 Msn Laboratories Limited Process for statins and its pharmaceutically acceptable salts thereof
ES2567171T3 (es) * 2006-10-09 2016-04-20 Msn Laboratories Private Limited Nuevo procedimiento para la preparación de estatinas y sus sales farmacéuticamente aceptables
JP2009531466A (ja) 2007-04-18 2009-09-03 テバ ファーマシューティカル インダストリーズ リミティド ＨＭＧ−ＣｏＡ還元酵素阻害剤の中間体の製造方法
EP2178890A1 (en) * 2007-07-12 2010-04-28 Teva Pharmaceutical Industries Ltd. Purification of rosuvastatin intermediate by thin film evaporation and chemical method
WO2010089770A2 (en) * 2009-01-19 2010-08-12 Msn Laboratories Limited Improved process for the preparation of highly pure (3r,5s)-7-[2-cyclopropyl-4-(4-fluorophenyl) quinolin-3-yl]-3,5-dihydroxy-6(e)-heptenoic acid and pharmaceutically acceptable salts thereof
KR101160152B1 (ko) * 2009-02-24 2012-06-27 한미사이언스 주식회사 스타틴 화합물 또는 그 염의 신규 제조방법, 및 이에 사용되는 중간체 화합물
EP2526099B1 (en) 2010-01-18 2016-03-30 MSN Laboratories Limited Improved process for the preparation of amide intermediates and their use thereof
WO2011104725A2 (en) * 2010-02-23 2011-09-01 Cadila Healthcare Limited Hmg-coa reductase inhibitors and process for the preparation thereof
EP2383260A3 (en) 2010-04-30 2011-12-28 Dipharma Francis S.r.l. Process for the preparation of statins
WO2011141934A1 (en) 2010-05-13 2011-11-17 Matrix Laboratories Ltd. An improved process for the preparation of an intermediate of hmg-coa reductase inhibitors
KR101292238B1 (ko) * 2010-07-01 2013-07-31 주식회사유한양행 ＨＭＧ-ＣｏＡ 환원효소 억제제 및 그의 중간체의 제조방법
EP3178812A1 (en) * 2010-11-12 2017-06-14 Hetero Research Foundation Novel polymorphs of pitavastatin calcium
EP2785851A2 (en) 2011-11-28 2014-10-08 Mylan Laboratories, Limited Process for producing chiral statin side chain intermediates employing candida antarctica lipase b
CN103288871A (zh) * 2012-02-28 2013-09-11 浙江京新药业股份有限公司 一种制备二羟基酸HMG-CoA还原酶抑制剂用的中间体及其制备方法和应用
ITVI20130039A1 (it) 2013-02-20 2014-08-21 F I S Fabbrica Italiana Sint I S P A Processo per la preparazione di intermedi chiave per la sintesi di statine
CN103172656B (zh) * 2013-04-02 2015-07-08 浙江科技学院 3-二甲基叔丁基硅氧基戊二酸酐的合成工艺
CN111518035A (zh) * 2020-06-18 2020-08-11 安徽鼎旺医药有限公司 一种瑞舒伐他汀叔丁胺盐及其制备方法
CN113683539B (zh) * 2021-09-23 2023-05-16 上海裕兰生物科技有限公司 一种聚酮中间体的合成方法

Family Cites Families (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5354772A (en) 1982-11-22 1994-10-11 Sandoz Pharm. Corp. Indole analogs of mevalonolactone and derivatives thereof
US4650890A (en) * 1984-04-03 1987-03-17 Sandoz Corp. Preparation of olefinic compounds and intermediates thereof
JP2569746B2 (ja) * 1987-08-20 1997-01-08 日産化学工業株式会社 キノリン系メバロノラクトン類
CA1336714C (en) 1987-08-20 1995-08-15 Yoshihiro Fujikawa Quinoline type mevalonolactone inhibitors of cholesterol biosynthesis
US4804770A (en) * 1988-04-29 1989-02-14 E. R. Squibb & Sons, Inc. Process for preparing a keto-phosphonate intermediate useful in preparing HMG-CoA reductase inhibitors
DE3911064A1 (de) 1989-04-06 1990-10-11 Bayer Ag Substituierte 1,8-naphthyridine
US5049577A (en) * 1990-01-29 1991-09-17 E. R. Squibb & Sons, Inc. 2-pyrrolidone substituted dihydroxy alkanoic, alkenoic and alkynoic acids, compositions and HMG-CoA reductase inhibition therewith
JP3528186B2 (ja) 1991-06-24 2004-05-17 日産化学工業株式会社 光学活性キノリンメバロン酸のジアステレオマー塩
AU3289102A (en) * 2000-11-16 2002-06-11 Teva Pharma Hydrolysis of (R(R*,R*))-2-(4-fluorophenyl)-beta,delta -dihydroxy-5-(1-methylethyl)-3-phenyl-4-((phenylamino) carbonyl)-1H-pyrrole-1-heptanoic acid esters with calcium hydroxide
WO2002063028A1 (fr) * 2001-02-02 2002-08-15 Mitsubishi Chemical Corporation Procede de production d'esters d'acide (3r,5s)-(e)-7-[2-cyclopropyl-4-(4-fluorophenyl)-quinolin-3-yl]-3,5-dihydroxyhept-6-enique
ES2364632T3 (es) * 2001-11-14 2011-09-08 Nissan Chemical Industries, Ltd. Procedimiento de producción de éster de ácido oxoheptenoico ópticamente activo.
US6835838B2 (en) * 2002-01-28 2004-12-28 Novartis Ag Process for the manufacture of organic compounds
GB0210234D0 (en) * 2002-05-03 2002-06-12 Novartis Ag Process for the manufacture of organic compounds

Also Published As

Publication number Publication date
WO2003064392A1 (en) 2003-08-07
PT1472228E (pt) 2009-06-24
ATE426594T1 (de) 2009-04-15
CA2472776A1 (en) 2003-08-07
CN1622937A (zh) 2005-06-01
JP4524111B2 (ja) 2010-08-11
EP1472228A1 (en) 2004-11-03
DE60326819D1 (de) 2009-05-07
CN1305853C (zh) 2007-03-21
NO327091B1 (no) 2009-04-20
EP1472228B1 (en) 2009-03-25
KR20040081161A (ko) 2004-09-20
ECSP045214A (es) 2004-09-28
BR0307303A (pt) 2005-01-11
ZA200405322B (en) 2005-07-27
AU2003226971B2 (en) 2006-11-30
ES2323267T3 (es) 2009-07-10
NZ534232A (en) 2006-03-31
US20050070605A1 (en) 2005-03-31
RU2299196C2 (ru) 2007-05-20
HK1070651A1 (en) 2005-06-24
MXPA04007396A (es) 2004-10-11
NO20043611L (no) 2004-08-30
PL370658A1 (en) 2005-05-30
JP2005520814A (ja) 2005-07-14
IL162980A (en) 2010-02-17
US7371865B2 (en) 2008-05-13
CA2472776C (en) 2011-01-25
US20080182873A1 (en) 2008-07-31
RU2004126442A (ru) 2005-06-10

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