BRPI0415681A - processo para a fabricação do sal de cálcio de ácido (e) -7-[4-(4-fluorofenil)-6-isopropil-2-[metil (metil sulfonil) amino] pirimidin-5-il] (3r, 5s) 3,5-dihidroxihept-6-enóico, composto, processo para formação de sal de cálcio de bis ([ácido (e)-7-[-4-(4-fluorofenil)-6-isopropil-2-[metil (metilsulfonil)amino] pirimidin-5-il](3r, 5s)-3,5-dihidroxihept-6-enóico], e, uso de um composto - Google Patents
processo para a fabricação do sal de cálcio de ácido (e) -7-[4-(4-fluorofenil)-6-isopropil-2-[metil (metil sulfonil) amino] pirimidin-5-il] (3r, 5s) 3,5-dihidroxihept-6-enóico, composto, processo para formação de sal de cálcio de bis ([ácido (e)-7-[-4-(4-fluorofenil)-6-isopropil-2-[metil (metilsulfonil)amino] pirimidin-5-il](3r, 5s)-3,5-dihidroxihept-6-enóico], e, uso de um compostoInfo
- Publication number
- BRPI0415681A BRPI0415681A BRPI0415681-1A BRPI0415681A BRPI0415681A BR PI0415681 A BRPI0415681 A BR PI0415681A BR PI0415681 A BRPI0415681 A BR PI0415681A BR PI0415681 A BRPI0415681 A BR PI0415681A
- Authority
- BR
- Brazil
- Prior art keywords
- methyl
- enoic
- fluorophenyl
- compound
- amino
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 6
- 159000000007 calcium salts Chemical class 0.000 title abstract 4
- 238000000034 method Methods 0.000 title abstract 4
- 238000004519 manufacturing process Methods 0.000 title abstract 3
- 230000015572 biosynthetic process Effects 0.000 title abstract 2
- 125000001255 4-fluorophenyl group Chemical group [H]C1=C([H])C(*)=C([H])C([H])=C1F 0.000 title 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 title 2
- 125000004170 methylsulfonyl group Chemical group [H]C([H])([H])S(*)(=O)=O 0.000 title 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 title 2
- 125000004528 pyrimidin-5-yl group Chemical group N1=CN=CC(=C1)* 0.000 title 2
- -1 4-FLUOROPHENYL Chemical class 0.000 abstract 3
- 239000002253 acid Substances 0.000 abstract 3
- NAWXUBYGYWOOIX-SFHVURJKSA-N (2s)-2-[[4-[2-(2,4-diaminoquinazolin-6-yl)ethyl]benzoyl]amino]-4-methylidenepentanedioic acid Chemical compound C1=CC2=NC(N)=NC(N)=C2C=C1CCC1=CC=C(C(=O)N[C@@H](CC(=C)C(O)=O)C(O)=O)C=C1 NAWXUBYGYWOOIX-SFHVURJKSA-N 0.000 abstract 1
- 229940121710 HMGCoA reductase inhibitor Drugs 0.000 abstract 1
- DHKHKXVYLBGOIT-UHFFFAOYSA-N acetaldehyde Diethyl Acetal Natural products CCOC(C)OCC DHKHKXVYLBGOIT-UHFFFAOYSA-N 0.000 abstract 1
- 125000002777 acetyl group Chemical class [H]C([H])([H])C(*)=O 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 abstract 1
- WCYWZMWISLQXQU-UHFFFAOYSA-N methyl Chemical class [CH3] WCYWZMWISLQXQU-UHFFFAOYSA-N 0.000 abstract 1
- 125000006239 protecting group Chemical group 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
- 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
- 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
-
- 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
-
- Y—GENERAL 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
- Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
- Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
- Y02P20/00—Technologies relating to chemical industry
- Y02P20/50—Improvements relating to the production of bulk chemicals
- Y02P20/55—Design 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)
- Veterinary Medicine (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Vascular Medicine (AREA)
- Heart & Thoracic Surgery (AREA)
- Cardiology (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
"PROCESSO PARA A FABRICAçãO DO SAL DE CáLCIO DE áCIDO (E)-7-¢4-(4-FLUOROFENIL)-6-ISOPROPIL-2-¢METIL(METIL SULFONIL)AMINO!PIR1MIDIN-5-IL!(3R,5S)-3,5-DIHIDROXIHEPT 6-ENóICO, COMPOSTO, PROCESSO PARA FORMAçãO DE SAL DE CáLCIO DE BIS (¢áCIDO (E)-7-¢4-(4-FLUOROFENIL)-6-ISOPROPIL-2¢METIL(METILSULFON IL)AMINO!PIRIMIDIN-5-IL!(3R,5S)-3,5DIHIDROXIHEPT-6-ENóIC O!, E, USO DE UM COMPOSTO". Processo para a fabricação de sal de cálcio de ácido (E)-7-¢4(4-fluorofenil)-6-isopropil-2-¢metil(metilsulfonil)amino!pirimidin-5 il!(3R,5S)-3,5-dihidroxihept-6-enóico, utilizável como um inibidor de HMGCoA reductase, a partir de um composto de fórmula (7), em que A é um grupo de proteção acetal ou cetal e R é alquila, via compostos cristalinos isolados de fórmula (8) ou fórmula (10) é descrito. Os intermediários cristalinos de fórmulas 7, 8 e 10 são também descritos.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB0324791.3A GB0324791D0 (en) | 2003-10-24 | 2003-10-24 | Chemical process |
| PCT/GB2004/004481 WO2005042522A1 (en) | 2003-10-24 | 2004-10-22 | Process for the manufacture of the calcium salt of rosuvatatin (e)-7-`4- (4-fluorophenyl) -6-isopropyl-2-`methyl (methylsulfonyl) amino ! pyrimidin -5-yl ! (3r, 5s) -3, 5-dihydroxyhept-6-enoic acid and crystalline intermediates thereof |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| BRPI0415681A true BRPI0415681A (pt) | 2006-12-19 |
Family
ID=29595716
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| BRPI0415681-1A BRPI0415681A (pt) | 2003-10-24 | 2004-10-22 | processo para a fabricação do sal de cálcio de ácido (e) -7-[4-(4-fluorofenil)-6-isopropil-2-[metil (metil sulfonil) amino] pirimidin-5-il] (3r, 5s) 3,5-dihidroxihept-6-enóico, composto, processo para formação de sal de cálcio de bis ([ácido (e)-7-[-4-(4-fluorofenil)-6-isopropil-2-[metil (metilsulfonil)amino] pirimidin-5-il](3r, 5s)-3,5-dihidroxihept-6-enóico], e, uso de um composto |
Country Status (28)
| Country | Link |
|---|---|
| US (2) | US20070255060A1 (pt) |
| EP (2) | EP1682536B1 (pt) |
| JP (3) | JP2007509119A (pt) |
| KR (1) | KR20060132829A (pt) |
| CN (2) | CN101654453B (pt) |
| AR (1) | AR046191A1 (pt) |
| AU (1) | AU2004285750B2 (pt) |
| BR (1) | BRPI0415681A (pt) |
| CA (1) | CA2543358A1 (pt) |
| CY (1) | CY1114145T1 (pt) |
| DK (1) | DK1682536T3 (pt) |
| ES (1) | ES2404693T3 (pt) |
| GB (1) | GB0324791D0 (pt) |
| IL (1) | IL175086A0 (pt) |
| IS (1) | IS8478A (pt) |
| MY (1) | MY146002A (pt) |
| NO (1) | NO20062263L (pt) |
| NZ (1) | NZ547094A (pt) |
| PL (1) | PL1682536T3 (pt) |
| PT (1) | PT1682536E (pt) |
| RU (1) | RU2372349C2 (pt) |
| SA (1) | SA04250425B1 (pt) |
| SI (1) | SI1682536T1 (pt) |
| TW (1) | TWI344957B (pt) |
| UA (1) | UA83076C2 (pt) |
| UY (1) | UY28577A1 (pt) |
| WO (1) | WO2005042522A1 (pt) |
| ZA (1) | ZA200603173B (pt) |
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| GB0003305D0 (en) | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
| GB0011120D0 (en) | 2000-05-09 | 2000-06-28 | Avecia Ltd | Process |
| NL1015744C2 (nl) | 2000-07-19 | 2002-01-22 | Dsm Nv | Werkwijze voor de bereiding van 2-(6-gesubstitueerde-1,3-dioxan-4-yl) azijnzuurderivaten. |
| IL159741A0 (en) | 2001-07-13 | 2004-06-20 | Astrazeneca Uk Ltd | Preparation of aminopyrimidine compounds |
| EP1323717A1 (en) | 2001-12-27 | 2003-07-02 | Dsm N.V. | Process for the preparation of 2-(6-Substituted-1,3-Dioxane-4-yL) acetic acid derivatives |
| EP1375493A1 (en) | 2002-06-17 | 2004-01-02 | Dsm N.V. | Process for the preparation of an dioxane acetic acid ester |
| GB0218781D0 (en) * | 2002-08-13 | 2002-09-18 | Astrazeneca Ab | Chemical process |
| DK1578731T3 (da) | 2002-12-16 | 2010-02-15 | Astrazeneca Uk Ltd | Fremgangsmåde til fremstilling af pyrimidinforbindelser |
| GB0312896D0 (en) * | 2003-06-05 | 2003-07-09 | Astrazeneca Ab | Chemical process |
| UY28501A1 (es) * | 2003-09-10 | 2005-04-29 | Astrazeneca Uk Ltd | Compuestos químicos |
| GB0322552D0 (en) | 2003-09-26 | 2003-10-29 | Astrazeneca Uk Ltd | Therapeutic treatment |
| GB0324791D0 (en) | 2003-10-24 | 2003-11-26 | Astrazeneca Ab | Chemical process |
| GB0428328D0 (en) * | 2004-12-24 | 2005-02-02 | Astrazeneca Uk Ltd | Chemical process |
| HU227120B1 (hu) * | 2005-05-26 | 2010-07-28 | Richter Gedeon Nyrt | Eljárás rosuvastatin kalciumsójának elõállítására új intermediereken keresztül |
| CN102807530B (zh) | 2005-06-24 | 2015-08-05 | 力奇制药公司 | 制备不含杂质的无定型罗苏伐他汀钙的方法 |
| GB0514078D0 (en) * | 2005-07-08 | 2005-08-17 | Astrazeneca Uk Ltd | Chemical process |
| US8455640B2 (en) | 2006-05-03 | 2013-06-04 | Msn Laboratories Limited | Process for statins and its pharmaceutically acceptable salts thereof |
| SI2086945T1 (sl) | 2006-10-09 | 2016-05-31 | Msn Laboratories Private Limited | Novi postopek za pripravo statinov in njihovih farmacevtsko sprejemljivih soli |
| US8318933B2 (en) * | 2006-10-31 | 2012-11-27 | Aurobindo Pharma Ltd | Process for preparing rosuvastatin calcium |
| TW200831469A (en) * | 2006-12-01 | 2008-08-01 | Astrazeneca Uk Ltd | Chemical process |
| ATE553098T1 (de) * | 2007-02-08 | 2012-04-15 | Aurobindo Pharma Ltd | Verfahren zur herstellung von rosuvastatin- calcium |
| JP2010501643A (ja) * | 2007-07-12 | 2010-01-21 | 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 | 薄膜蒸発及び化学的手法によるロスバスタチン中間体の精製 |
| EP2022784A1 (en) | 2007-08-08 | 2009-02-11 | LEK Pharmaceuticals D.D. | Process for the preparation of methyl ester of rosuvastatin |
| US8793497B2 (en) * | 2008-05-09 | 2014-07-29 | Qualcomm Incorporated | Puzzle-based authentication between a token and verifiers |
| EP2298745B1 (en) | 2008-05-27 | 2014-09-03 | Changzhou Pharmaceutical Factory | Preparation method of rosuvastatin calcium and its intermediates |
| EA021942B1 (ru) | 2009-01-15 | 2015-10-30 | Эгиш Дьёдьсердьяр Зрт. | Способ изготовления солей розувастатина |
| EP2387561A4 (en) | 2009-01-19 | 2012-07-25 | Msn Lab Ltd | IMPROVED METHOD FOR THE PRODUCTION OF HIGH-PURITY (3R, 5S) -7- [2-CYCLOPROPYL-4- (4-FLUORPHENYL) CHINOLIN-3-YL] -3,5-DIHYDROXY-6 (E) -HEPTENIC ACID AND PHARMACEUTICAL ACCEPTABLE SALTS THEREOF |
| WO2011021058A1 (en) * | 2009-08-17 | 2011-02-24 | Aurobindo Pharma Limited | Process for the manufacture of rosuvastatin calcium using crystalline rosuvastatin ethyl ester |
| EP2336116A1 (en) * | 2009-12-16 | 2011-06-22 | LEK Pharmaceuticals d.d. | Process for the preparation of key intermediates for the synthesis of rosuvastatin or pharmaceutically acceptable salts thereof |
| US8987444B2 (en) | 2010-01-18 | 2015-03-24 | Msn Laboratories Private Limited | Process for the preparation of amide intermediates and their use thereof |
| CN102219749B (zh) * | 2010-04-14 | 2013-07-17 | 上海京新生物医药有限公司 | 一种制备瑞苏伐他汀钙的方法 |
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| EP2588474A4 (en) * | 2010-07-01 | 2014-07-23 | Yuhan Corp | PROCESS FOR THE PREPARATION OF HMG-COA REDUCTASE INHIBITORS AND INTERMEDIATE PRODUCTS THEREOF |
| HU230987B1 (hu) * | 2010-11-29 | 2019-08-28 | Egis Gyógyszergyár Nyrt. | Eljárás nagy tisztaságú gyógyszeripari intermedierek előállítására |
| CN103313983B (zh) * | 2011-01-18 | 2016-06-29 | 中化帝斯曼制药有限公司荷兰公司 | 在碱存在下制备他汀类化合物的方法 |
| CN103848790B (zh) * | 2012-12-05 | 2016-08-03 | 安徽省庆云医药化工有限公司 | 瑞舒伐他汀酯的晶型及其制备方法 |
| CN103724278B (zh) * | 2013-12-12 | 2019-03-29 | 江苏阿尔法药业有限公司 | 他汀类中间体及其衍生物的制备方法 |
| EP3103878A4 (en) | 2014-02-06 | 2017-08-16 | API Corporation | Rosuvastatin calcium and process for producing intermediate thereof |
| CN105153040B (zh) * | 2015-10-15 | 2018-04-13 | 江苏师范大学 | 瑞舒伐他汀钙新晶型及其制备方法 |
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| NL1015744C2 (nl) * | 2000-07-19 | 2002-01-22 | Dsm Nv | Werkwijze voor de bereiding van 2-(6-gesubstitueerde-1,3-dioxan-4-yl) azijnzuurderivaten. |
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