MX343273B - Intermediarios clave para la sintesis de rosuvastatina o de sales farmaceuticamente aceptables de la misma. - Google Patents
Intermediarios clave para la sintesis de rosuvastatina o de sales farmaceuticamente aceptables de la misma.Info
- Publication number
- MX343273B MX343273B MX2011007990A MX2011007990A MX343273B MX 343273 B MX343273 B MX 343273B MX 2011007990 A MX2011007990 A MX 2011007990A MX 2011007990 A MX2011007990 A MX 2011007990A MX 343273 B MX343273 B MX 343273B
- Authority
- MX
- Mexico
- Prior art keywords
- rosuvastatin
- synthesis
- pharmaceutically acceptable
- acceptable salts
- key intermediates
- Prior art date
Links
- 239000000543 intermediate Substances 0.000 title abstract 2
- BPRHUIZQVSMCRT-VEUZHWNKSA-N rosuvastatin Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1\C=C\[C@@H](O)C[C@@H](O)CC(O)=O BPRHUIZQVSMCRT-VEUZHWNKSA-N 0.000 title abstract 2
- 229960000672 rosuvastatin Drugs 0.000 title abstract 2
- 230000015572 biosynthetic process Effects 0.000 title 1
- 150000003839 salts Chemical class 0.000 title 1
- 238000003786 synthesis reaction Methods 0.000 title 1
- MSDYDUNHTAYBHV-UHFFFAOYSA-N n-[4-(4-fluorophenyl)-5-(hydroxymethyl)-6-propan-2-ylpyrimidin-2-yl]-n-methylmethanesulfonamide Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1CO MSDYDUNHTAYBHV-UHFFFAOYSA-N 0.000 abstract 1
- VZTXNOOWMMDDLR-UHFFFAOYSA-N n-[4-(4-fluorophenyl)-5-methyl-6-propan-2-ylpyrimidin-2-yl]-n-methylmethanesulfonamide Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C=CC(F)=CC=2)=C1C VZTXNOOWMMDDLR-UHFFFAOYSA-N 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
- C07D239/02—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings
- C07D239/24—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more double bonds between ring members or between ring members and non-ring members
- C07D239/28—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings not condensed with other rings having three or more 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, directly attached to ring carbon atoms
- C07D239/32—One oxygen, sulfur or nitrogen atom
- C07D239/42—One nitrogen atom
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
-
- 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
-
- 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
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/535—Organo-phosphoranes
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F9/00—Compounds containing elements of Groups 5 or 15 of the Periodic Table
- C07F9/02—Phosphorus compounds
- C07F9/28—Phosphorus compounds with one or more P—C bonds
- C07F9/54—Quaternary phosphonium compounds
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Biochemistry (AREA)
- Molecular Biology (AREA)
- Obesity (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Hematology (AREA)
- Diabetes (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente invención se refiere en general al campo de la química orgánica, y en particular a la preparación de la N-(4-(4-fluoro-fenil)-6-isopropil-5-metil-pirimidin-2-il)-N-metil -metan-sulfonamida (I), de la N-(4-(4-fluoro-fenil)-5-(bromo-metil )-6-iso-propil-pirimidin-2-il)-N-metil-metan-sulfonamida (II), y de la N-(4-(4-fIuoro-fenil)-5-(hidroxi-metil)-6-isopropil-pirimidi n-2-il)-N-metil-metan-sulfonamida (III), como los intermediarios clave en la preparación de la rosuvastatina.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP09151881A EP2264015A1 (en) | 2009-02-02 | 2009-02-02 | Key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof |
| PCT/EP2010/051163 WO2010086438A1 (en) | 2009-02-02 | 2010-02-01 | Key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2011007990A MX2011007990A (es) | 2011-09-06 |
| MX343273B true MX343273B (es) | 2016-10-31 |
Family
ID=40589996
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2011007990A MX343273B (es) | 2009-02-02 | 2010-02-01 | Intermediarios clave para la sintesis de rosuvastatina o de sales farmaceuticamente aceptables de la misma. |
Country Status (10)
| Country | Link |
|---|---|
| US (2) | US20120022091A1 (es) |
| EP (2) | EP2264015A1 (es) |
| JP (1) | JP5558492B2 (es) |
| CN (1) | CN102365272B (es) |
| AU (1) | AU2010209650B2 (es) |
| BR (1) | BRPI1007151A2 (es) |
| CA (1) | CA2750801C (es) |
| EA (1) | EA021733B1 (es) |
| MX (1) | MX343273B (es) |
| WO (1) | WO2010086438A1 (es) |
Families Citing this family (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP2423195A1 (en) * | 2010-07-26 | 2012-02-29 | LEK Pharmaceuticals d.d. | Process for the preparation of key intermediates for the synthesis of statins or pharmaceutically acceptable salts thereof |
| ES2601479T3 (es) | 2011-01-18 | 2017-02-15 | Dsm Sinochem Pharmaceuticals Netherlands B.V. | Proceso para la preparación de diolsulfonas |
| CN102311457B (zh) * | 2011-09-16 | 2014-04-16 | 苏州莱克施德药业有限公司 | 罗苏伐他汀的制备方法 |
| CN102936225A (zh) * | 2012-11-15 | 2013-02-20 | 江苏阿尔法药业有限公司 | 一种含溴甲基、羟甲基或甲酰基的瑞舒伐他汀钙中间体的制备方法 |
| CN103420919B (zh) * | 2013-08-22 | 2015-07-08 | 南京欧信医药技术有限公司 | 一种嘧啶类衍生物的合成方法 |
| CN105175346B (zh) * | 2015-05-19 | 2018-02-06 | 上海弈柯莱生物医药科技有限公司 | 一种合成瑞舒伐他汀钙中间体的方法 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2648897B2 (ja) | 1991-07-01 | 1997-09-03 | 塩野義製薬株式会社 | ピリミジン誘導体 |
| WO2005054207A1 (en) * | 2003-12-04 | 2005-06-16 | Glenmark Pharmaceuticals Limited | Process for the preparation of pyrimidine derivatives |
| US8354530B2 (en) | 2005-07-28 | 2013-01-15 | Lek Pharmaceuticals d. d | Process for the synthesis of rosuvastatin calcium |
| EP1775299A1 (en) * | 2005-10-05 | 2007-04-18 | LEK Pharmaceuticals D.D. | Process for the synthesis of HMG-CoA reductase inhibitors |
| WO2008059519A2 (en) | 2006-09-25 | 2008-05-22 | Glenmark Pharmaceuticals Limited | A process for the preparation of intermediates of rosuvastatin |
| US8183397B2 (en) * | 2007-04-03 | 2012-05-22 | Lek Pharmaceuticals D.D. | Synthesis of statins |
-
2009
- 2009-02-02 EP EP09151881A patent/EP2264015A1/en not_active Ceased
-
2010
- 2010-02-01 US US13/145,783 patent/US20120022091A1/en not_active Abandoned
- 2010-02-01 JP JP2011546865A patent/JP5558492B2/ja not_active Expired - Fee Related
- 2010-02-01 BR BRPI1007151A patent/BRPI1007151A2/pt not_active IP Right Cessation
- 2010-02-01 CN CN201080014893.5A patent/CN102365272B/zh not_active Expired - Fee Related
- 2010-02-01 MX MX2011007990A patent/MX343273B/es active IP Right Grant
- 2010-02-01 EP EP10703830.9A patent/EP2391609B1/en not_active Not-in-force
- 2010-02-01 AU AU2010209650A patent/AU2010209650B2/en not_active Ceased
- 2010-02-01 EA EA201101150A patent/EA021733B1/ru not_active IP Right Cessation
- 2010-02-01 WO PCT/EP2010/051163 patent/WO2010086438A1/en active Application Filing
- 2010-02-01 CA CA2750801A patent/CA2750801C/en not_active Expired - Fee Related
-
2015
- 2015-01-29 US US14/609,248 patent/US9376397B2/en active Active
Also Published As
| Publication number | Publication date |
|---|---|
| AU2010209650A1 (en) | 2011-08-25 |
| US20150141449A1 (en) | 2015-05-21 |
| JP5558492B2 (ja) | 2014-07-23 |
| AU2010209650B2 (en) | 2015-09-17 |
| EA021733B1 (ru) | 2015-08-31 |
| CA2750801A1 (en) | 2010-08-05 |
| EA201101150A1 (ru) | 2012-03-30 |
| CN102365272B (zh) | 2014-07-16 |
| MX2011007990A (es) | 2011-09-06 |
| JP2012516839A (ja) | 2012-07-26 |
| US20120022091A1 (en) | 2012-01-26 |
| EP2264015A1 (en) | 2010-12-22 |
| CN102365272A (zh) | 2012-02-29 |
| US9376397B2 (en) | 2016-06-28 |
| EP2391609A1 (en) | 2011-12-07 |
| BRPI1007151A2 (pt) | 2016-02-23 |
| WO2010086438A1 (en) | 2010-08-05 |
| CA2750801C (en) | 2017-08-29 |
| EP2391609B1 (en) | 2015-01-28 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FG | Grant or registration |