CY1115040T1 - Διαδικασια και ενδιaμεσες ενωσεις χρησιμες στην παρασκευη στατινων (sτατινs), ειδικοτερα rosuvasτατιν - Google Patents
Διαδικασια και ενδιaμεσες ενωσεις χρησιμες στην παρασκευη στατινων (sτατινs), ειδικοτερα rosuvasτατινInfo
- Publication number
- CY1115040T1 CY1115040T1 CY20121100274T CY121100274T CY1115040T1 CY 1115040 T1 CY1115040 T1 CY 1115040T1 CY 20121100274 T CY20121100274 T CY 20121100274T CY 121100274 T CY121100274 T CY 121100274T CY 1115040 T1 CY1115040 T1 CY 1115040T1
- Authority
- CY
- Cyprus
- Prior art keywords
- formula
- compound
- group
- protecting
- protecting group
- Prior art date
Links
Classifications
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- 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
-
- 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
- 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
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/02—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
- C07D309/08—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having no 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
- C07D309/10—Oxygen atoms
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D309/00—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
- C07D309/16—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
- C07D309/28—Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member 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
- C07D309/30—Oxygen atoms, e.g. delta-lactones
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- 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)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Urology & Nephrology (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Obesity (AREA)
- Vascular Medicine (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Plural Heterocyclic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Pyrane Compounds (AREA)
- Steroid Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Abstract
Παρέχεται μία διαδικασία για την Παρασκευή μιας ένωσης του τύπου (7): τύπος (7) όπου το R1 αντιπροσωπεύει μία ομάδα αλκυλίου (alkyl), το R2 αντιπροσωπεύει μία ομάδα αρυλίου (aryl), το R3 αντιπροσωπεύει υδρογόνο, μία προστατευτική ομάδα ή μία ομάδα αλκυλίου (alkyl), και το R4 αντιπροσωπεύει υδρογόνο, μία προστατευτική ομάδα ή μία ομάδα SΟ2R5 όπου το R5 είναι μία ομάδα αλκυλίου (alkyl), που περιλαμβάνει a) υδροξυλίωση μιας ένωσης του τύπου (1): τύπος (1), όπου το Υ αντιπροσωπεύει μία ομάδα αλογόνου, το Ρ1 αντιπροσωπεύει υδρογόνο ή μία προστατευτική ομάδα, και το W αντιπροσωπεύει =O ή -ΟΡ2, στο οποίο το Ρ2 αντιπροσωπεύει υδρογόνο ή μία προστατευτική ομάδα, ώστε να δώσει μία ένωση του τύπου (2): τύπος (2) b) οξείδωση της ένωσης του τύπου (2) ώστε να δώσει μία ένωση του τύπου (3): τύπος (3) c) σύνδεση της ένωσης του τύπου (3) με μία ένωση του τύπου (4): τύπος (4) όπου το R3 αντιπροσωπεύει μία προστατευτική ομάδα ή μία ομάδα αλκυλίου (alkyl), το R4 αντιπροσωπεύει μία προστατευτική ομάδα ή μία ομάδα SΟ2R5 όπου το R5 είναι μία ομάδα αλκυλίου (alkyl), όπως μία ομάδα C1-6 alkyl, και το R6 αντιπροσωπεύει (ΡR7R8)+Χ ή Ρ(=Ο)R7R8 στο οποίο το Χ είναι ένα ανιόν και τα R7 και R8 το καθένα ανεξάρτητα είναι ένα αλκύλιο (alkyl), αρύλιο (aryl), ομάδα alkoxy ή aryloxy, ώστε να δώσει μία ένωση του τύπου (5): τύπος (5) όπου το R3 αντιπροσωπεύει μία προστατευτική ομάδα ή μία ομάδα αλκυλίου (alkyl), και το R4 αντιπροσωπεύει μία προστατευτική ομάδα ή μία ομάδα SΟ2R5 όπου το R5 είναι μία ομάδα αλκυλίου (alkyl), d) όταν το W αντιπροσωπεύει -ΟΡ2, απομάκρυνση οποιασδήποτε προστατευτικής ομάδας Ρ2 και οξείδωση της ένωσης του τύπου (5) ώστε να δώσει μία ένωση του τύπου (6): τύπος (6) και e) υποβολή της ένωσης του τύπου (5) όταν το W αντιπροσωπεύει =O, ή μία ένωση του τύπου (6) σε άνοιγμα δακτυλίου, απομάκρυνση οποιωνδήποτε προστατευτικών ομάδων Ρ1, και προαιρετικά απομάκρυνση οποιωνδήποτε πρόσθετων προστατευτικών
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GB0406757A GB0406757D0 (en) | 2004-03-26 | 2004-03-26 | Process and compounds |
| EP20080157487 EP1958633B1 (en) | 2004-03-26 | 2005-03-23 | Process and intermediate compounds useful in the preparation of statins, particularly rosuvastatin |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CY1115040T1 true CY1115040T1 (el) | 2016-12-14 |
Family
ID=32188702
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY101100456T CY1110091T1 (el) | 2004-03-26 | 2010-05-21 | Διεργασια και ενδιαμεσες ενωσεις χρησιμες κατα την παρασκευη στατινων, ιδιαιτερα της ροσουβαστατινης |
| CY20121100274T CY1115040T1 (el) | 2004-03-26 | 2012-03-14 | Διαδικασια και ενδιaμεσες ενωσεις χρησιμες στην παρασκευη στατινων (sτατινs), ειδικοτερα rosuvasτατιν |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CY101100456T CY1110091T1 (el) | 2004-03-26 | 2010-05-21 | Διεργασια και ενδιαμεσες ενωσεις χρησιμες κατα την παρασκευη στατινων, ιδιαιτερα της ροσουβαστατινης |
Country Status (21)
| Country | Link |
|---|---|
| US (2) | US8703945B2 (el) |
| EP (2) | EP1729775B1 (el) |
| JP (1) | JP5016478B2 (el) |
| KR (1) | KR20060130765A (el) |
| CN (1) | CN101022807B (el) |
| AT (2) | ATE536875T1 (el) |
| AU (1) | AU2005225602A1 (el) |
| BR (1) | BRPI0507999A (el) |
| CA (1) | CA2561059C (el) |
| CY (2) | CY1110091T1 (el) |
| DE (1) | DE602005019547D1 (el) |
| DK (2) | DK1958633T3 (el) |
| ES (2) | ES2341658T3 (el) |
| GB (1) | GB0406757D0 (el) |
| HR (1) | HRP20100287T1 (el) |
| IL (1) | IL178274A0 (el) |
| PL (2) | PL1729775T3 (el) |
| PT (2) | PT1729775E (el) |
| RS (1) | RS51306B (el) |
| SI (2) | SI1729775T1 (el) |
| WO (1) | WO2005092867A2 (el) |
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| HUP0401248A3 (en) | 2001-07-13 | 2004-11-29 | Astrazeneca Uk Ltd | Preparation of aminopyrimidine compounds and new intermediates |
| GB0218781D0 (en) | 2002-08-13 | 2002-09-18 | Astrazeneca Ab | Chemical process |
| GB0312896D0 (en) | 2003-06-05 | 2003-07-09 | Astrazeneca Ab | Chemical process |
| GB0324791D0 (en) | 2003-10-24 | 2003-11-26 | Astrazeneca Ab | Chemical process |
| GB0406757D0 (en) * | 2004-03-26 | 2004-04-28 | Avecia Ltd | Process and compounds |
| GB0427491D0 (en) * | 2004-12-16 | 2005-01-19 | Avecia Ltd | Process and compounds |
| CA2612587C (en) * | 2005-06-24 | 2013-02-19 | Lek Pharmaceuticals D.D. | Process for preparing amorphous rosuvastatin calcium free of impurities |
| US8183397B2 (en) | 2007-04-03 | 2012-05-22 | Lek Pharmaceuticals D.D. | Synthesis of statins |
| EP1978020A1 (en) * | 2007-04-03 | 2008-10-08 | LEK Pharmaceuticals D.D. | Processes for the preparation of statins, particularly rosuvastatin, and intermediates for the preparation thereof |
| US8404870B2 (en) | 2008-01-23 | 2013-03-26 | Lek Pharmaceuticals D.D. | ((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)methyl carboxylate and process for the production thereof |
| GB0904102D0 (en) * | 2009-03-10 | 2009-04-22 | Bradford Pharma Ltd | Use of atorvastatin lactols as medicaments |
| GB0904100D0 (en) * | 2009-03-10 | 2009-04-22 | Bradford Pharma Ltd | Use of rosuvastatin lactols as medicaments |
| AU2013202895B2 (en) * | 2009-03-10 | 2014-09-18 | Redx Pharma Plc | Rosuvastatin and atorvastatin derivatives |
| GB0904104D0 (en) * | 2009-03-10 | 2009-04-22 | Bradford Pharma Ltd | Atorvastatin and rosuvastatin derivatives |
Family Cites Families (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4474971A (en) * | 1982-09-29 | 1984-10-02 | Sandoz, Inc. | (Tetrahydropyran-2-yl)-aldehydes |
| US4625039A (en) | 1983-12-21 | 1986-11-25 | Sandoz Pharm. Corp. | 4-trisubstituted silyl protected hydroxy-6-oxo-tetrahydropyran-2-yl-aldehyde intermediates |
| US4677211A (en) * | 1984-06-29 | 1987-06-30 | Sandoz Pharmaceuticals Corp. | Preparation of lactones |
| 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 |
| US5795749A (en) | 1995-04-05 | 1998-08-18 | The Scripps Research Institution | Use of 2-deoxyribose-5-phosphate aldolase to prepare 2-deoxyfucose, analogues and derivatives |
| GB9903472D0 (en) | 1999-02-17 | 1999-04-07 | Zeneca Ltd | Chemical process |
| AU7717500A (en) * | 1999-09-30 | 2001-04-30 | Merck & Co., Inc. | Anti-hypercholesterolemic drug combination |
| GB0003305D0 (en) | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
| GB0011163D0 (en) * | 2000-05-10 | 2000-06-28 | Astrazeneca Ab | Chemical compound |
| WO2003026573A2 (en) * | 2001-09-24 | 2003-04-03 | Merck & Co., Inc. | Screening and selection methods for statin drug combinations |
| DE10216967A1 (de) * | 2002-04-16 | 2003-11-13 | Bayer Ag | Verfahren zur Herstellung spezieller aromatischer Aldehyde |
| US7371759B2 (en) * | 2003-09-25 | 2008-05-13 | Bristol-Myers Squibb Company | HMG-CoA reductase inhibitors and method |
| WO2005040134A1 (en) * | 2003-10-22 | 2005-05-06 | Ranbaxy Laboratories Limited | Process for the preparation of amorphous rosuvastatin calcium |
| DE10352659B4 (de) | 2003-11-11 | 2007-09-13 | Ratiopharm Gmbh | Verfahren zur Herstellung von Statinen und Tetrahydropyranonderivate zur Verwendung in dem Verfahren |
| GB0406757D0 (en) * | 2004-03-26 | 2004-04-28 | Avecia Ltd | Process and compounds |
-
2004
- 2004-03-26 GB GB0406757A patent/GB0406757D0/en not_active Ceased
-
2005
- 2005-03-23 DK DK08157487T patent/DK1958633T3/da active
- 2005-03-23 SI SI200531001T patent/SI1729775T1/sl unknown
- 2005-03-23 JP JP2007504474A patent/JP5016478B2/ja not_active Expired - Fee Related
- 2005-03-23 SI SI200531491T patent/SI1958633T1/sl unknown
- 2005-03-23 EP EP20050731809 patent/EP1729775B1/en active Active
- 2005-03-23 US US10/594,380 patent/US8703945B2/en not_active Expired - Fee Related
- 2005-03-23 KR KR20067021900A patent/KR20060130765A/ko not_active Application Discontinuation
- 2005-03-23 ES ES05731809T patent/ES2341658T3/es active Active
- 2005-03-23 EP EP20080157487 patent/EP1958633B1/en not_active Not-in-force
- 2005-03-23 PL PL05731809T patent/PL1729775T3/pl unknown
- 2005-03-23 BR BRPI0507999-3A patent/BRPI0507999A/pt not_active Application Discontinuation
- 2005-03-23 AT AT08157487T patent/ATE536875T1/de active
- 2005-03-23 RS RSP20100217 patent/RS51306B/sr unknown
- 2005-03-23 PT PT05731809T patent/PT1729775E/pt unknown
- 2005-03-23 WO PCT/GB2005/001099 patent/WO2005092867A2/en active Application Filing
- 2005-03-23 PL PL08157487T patent/PL1958633T3/pl unknown
- 2005-03-23 DE DE200560019547 patent/DE602005019547D1/de active Active
- 2005-03-23 PT PT08157487T patent/PT1958633E/pt unknown
- 2005-03-23 ES ES08157487T patent/ES2379481T3/es active Active
- 2005-03-23 DK DK05731809T patent/DK1729775T3/da active
- 2005-03-23 CN CN2005800096821A patent/CN101022807B/zh not_active Expired - Fee Related
- 2005-03-23 AU AU2005225602A patent/AU2005225602A1/en not_active Abandoned
- 2005-03-23 CA CA 2561059 patent/CA2561059C/en not_active Expired - Fee Related
- 2005-03-23 AT AT05731809T patent/ATE458484T1/de active
-
2006
- 2006-09-25 IL IL178274A patent/IL178274A0/en unknown
-
2010
- 2010-05-21 CY CY101100456T patent/CY1110091T1/el unknown
- 2010-05-21 HR HR20100287T patent/HRP20100287T1/hr unknown
-
2012
- 2012-03-14 CY CY20121100274T patent/CY1115040T1/el unknown
-
2014
- 2014-03-25 US US14/225,018 patent/US9024025B2/en not_active Expired - Fee Related
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