ATE536875T1 - Verfahren und zwischenzusammensetzungen zur herstellung von statinen, insbesondere rosuvastatin - Google Patents

Verfahren und zwischenzusammensetzungen zur herstellung von statinen, insbesondere rosuvastatin

Info

Publication number: ATE536875T1
Authority: AT; Austria
Prior art keywords: formula; compound; group; protecting; protecting group
Prior art date: 2004-03-26

Application number

AT08157487T

Other languages

English (en)

Inventor

David John Moody

Jonathan William Wiffen

Original Assignee

Bradford Pharma Ltd

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.)

2004-03-26

Filing date

2005-03-23

Publication date

2011-12-15

2005-03-23 Application filed by Bradford Pharma Ltd filed Critical Bradford Pharma Ltd

2011-12-15 Application granted granted Critical

2011-12-15 Publication of ATE536875T1 publication Critical patent/ATE536875T1/de

Links

238000000034 method Methods 0.000 title abstract 2
229940121710 HMGCoA reductase inhibitor Drugs 0.000 title 1
239000002471 hydroxymethylglutaryl coenzyme A reductase inhibitor Substances 0.000 title 1
239000000203 mixture Substances 0.000 title 1
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 1
229960000672 rosuvastatin Drugs 0.000 title 1
150000001875 compounds Chemical class 0.000 abstract 13
125000006239 protecting group Chemical group 0.000 abstract 10
125000000217 alkyl group Chemical group 0.000 abstract 8
229910052739 hydrogen Inorganic materials 0.000 abstract 4
239000001257 hydrogen Substances 0.000 abstract 4
UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 abstract 2
125000003118 aryl group Chemical group 0.000 abstract 2
150000002431 hydrogen Chemical class 0.000 abstract 2
125000003545 alkoxy group Chemical group 0.000 abstract 1
150000001450 anions Chemical group 0.000 abstract 1
125000004104 aryloxy group Chemical group 0.000 abstract 1
230000008878 coupling Effects 0.000 abstract 1
238000010168 coupling process Methods 0.000 abstract 1
238000005859 coupling reaction Methods 0.000 abstract 1
125000005843 halogen group Chemical group 0.000 abstract 1
230000000640 hydroxylating effect Effects 0.000 abstract 1
238000007142 ring opening reaction Methods 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
- 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
- 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)
Public Health (AREA)
General Health & Medical Sciences (AREA)
Veterinary Medicine (AREA)
Chemical Kinetics & Catalysis (AREA)
General Chemical & Material Sciences (AREA)
Medicinal Chemistry (AREA)
Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
Pharmacology & Pharmacy (AREA)
Life Sciences & Earth Sciences (AREA)
Animal Behavior & Ethology (AREA)
Obesity (AREA)
Diabetes (AREA)
Urology & Nephrology (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)
Plural Heterocyclic Compounds (AREA)
Pyrane Compounds (AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Steroid Compounds (AREA)

AT08157487T 2004-03-26 2005-03-23 Verfahren und zwischenzusammensetzungen zur herstellung von statinen, insbesondere rosuvastatin ATE536875T1 (de)

Applications Claiming Priority (1)

Application Number	Priority Date	Filing Date	Title
GB0406757A GB0406757D0 (en)	2004-03-26	2004-03-26	Process and compounds

Publications (1)

Publication Number	Publication Date
ATE536875T1 true ATE536875T1 (de)	2011-12-15

Family

ID=32188702

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
AT05731809T ATE458484T1 (de)	2004-03-26	2005-03-23	ßVERFAHREN UND ZWISCHENPRODUKTE ZUR HERSTELLUNG VON STATINEN; INSBESONDERE VON ROSUVASTATINß
AT08157487T ATE536875T1 (de)	2004-03-26	2005-03-23	Verfahren und zwischenzusammensetzungen zur herstellung von statinen, insbesondere rosuvastatin

Family Applications Before (1)

Application Number	Title	Priority Date	Filing Date
AT05731809T ATE458484T1 (de)	2004-03-26	2005-03-23	ßVERFAHREN UND ZWISCHENPRODUKTE ZUR HERSTELLUNG VON STATINEN; INSBESONDERE VON ROSUVASTATINß

Country Status (21)

Country	Link
US (2)	US8703945B2 (de)
EP (2)	EP1958633B1 (de)
JP (1)	JP5016478B2 (de)
KR (1)	KR20060130765A (de)
CN (1)	CN101022807B (de)
AT (2)	ATE458484T1 (de)
AU (1)	AU2005225602A1 (de)
BR (1)	BRPI0507999A (de)
CA (1)	CA2561059C (de)
CY (2)	CY1110091T1 (de)
DE (1)	DE602005019547D1 (de)
DK (2)	DK1958633T3 (de)
ES (2)	ES2379481T3 (de)
GB (1)	GB0406757D0 (de)
HR (1)	HRP20100287T1 (de)
IL (1)	IL178274A0 (de)
PL (2)	PL1729775T3 (de)
PT (2)	PT1958633E (de)
RS (1)	RS51306B (de)
SI (2)	SI1729775T1 (de)
WO (1)	WO2005092867A2 (de)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
KR100888408B1 (ko)	2001-07-13	2009-03-13	아스트라제네카 유케이 리미티드	아미노피리미딘 화합물의 제조 방법
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
EP2508514B1 (de) *	2005-06-24	2017-10-18	LEK Pharmaceuticals d.d.	Verfahren zur Herstellung von amorphem Rosuvastatincalcium frei von Verunreinigungen
EP1978020A1 (de) *	2007-04-03	2008-10-08	LEK Pharmaceuticals D.D.	Verfahren zur Herstellung von Statinen, insbesondere von Rosuvastatin, und Zwischenprodukt für deren Herstellung
WO2008119810A2 (en)	2007-04-03	2008-10-09	Lek Pharmaceuticals D.D.	Processes for the preparation of statins, particularly rosuvastatin, and intermediates for the preparation thereof
WO2009092702A2 (en)	2008-01-23	2009-07-30	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
GB0904104D0 (en) *	2009-03-10	2009-04-22	Bradford Pharma Ltd	Atorvastatin and rosuvastatin derivatives
AU2013202895B2 (en) *	2009-03-10	2014-09-18	Redx Pharma Plc	Rosuvastatin and atorvastatin derivatives
GB0904100D0 (en)	2009-03-10	2009-04-22	Bradford Pharma Ltd	Use of rosuvastatin lactols as medicaments

Family Cites Families (15)

* Cited by examiner, † Cited by third party
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
WO2001022962A1 (en) *	1999-09-30	2001-04-05	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
JP2005512516A (ja) *	2001-09-24	2005-05-12	メルク　エンド　カムパニー　インコーポレーテッド	スタチン薬物の組合せのスクリーニング方法および選択方法
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
EP1678148A1 (de) *	2003-10-22	2006-07-12	Ranbaxy Laboratories Limited	Verfahren zur herstellung von amorphen 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 US US10/594,380 patent/US8703945B2/en not_active Expired - Fee Related
- 2005-03-23 SI SI200531001T patent/SI1729775T1/sl unknown
- 2005-03-23 AU AU2005225602A patent/AU2005225602A1/en not_active Abandoned
- 2005-03-23 CN CN2005800096821A patent/CN101022807B/zh not_active Expired - Fee Related
- 2005-03-23 PT PT08157487T patent/PT1958633E/pt unknown
- 2005-03-23 EP EP20080157487 patent/EP1958633B1/de not_active Expired - Lifetime
- 2005-03-23 EP EP20050731809 patent/EP1729775B1/de not_active Expired - Lifetime
- 2005-03-23 WO PCT/GB2005/001099 patent/WO2005092867A2/en not_active Ceased
- 2005-03-23 DE DE200560019547 patent/DE602005019547D1/de not_active Expired - Lifetime
- 2005-03-23 RS RSP20100217 patent/RS51306B/sr unknown
- 2005-03-23 PT PT05731809T patent/PT1729775E/pt unknown
- 2005-03-23 ES ES08157487T patent/ES2379481T3/es not_active Expired - Lifetime
- 2005-03-23 SI SI200531491T patent/SI1958633T1/sl unknown
- 2005-03-23 HR HR20100287T patent/HRP20100287T1/hr unknown
- 2005-03-23 JP JP2007504474A patent/JP5016478B2/ja not_active Expired - Fee Related
- 2005-03-23 PL PL05731809T patent/PL1729775T3/pl unknown
- 2005-03-23 PL PL08157487T patent/PL1958633T3/pl unknown
- 2005-03-23 CA CA 2561059 patent/CA2561059C/en not_active Expired - Fee Related
- 2005-03-23 DK DK08157487T patent/DK1958633T3/da active
- 2005-03-23 AT AT05731809T patent/ATE458484T1/de active
- 2005-03-23 BR BRPI0507999-3A patent/BRPI0507999A/pt not_active Application Discontinuation
- 2005-03-23 KR KR20067021900A patent/KR20060130765A/ko not_active Withdrawn
- 2005-03-23 AT AT08157487T patent/ATE536875T1/de active
- 2005-03-23 ES ES05731809T patent/ES2341658T3/es not_active Expired - Lifetime
- 2005-03-23 DK DK05731809T patent/DK1729775T3/da active
2006
- 2006-09-25 IL IL178274A patent/IL178274A0/en unknown
2010
- 2010-05-21 CY CY101100456T patent/CY1110091T1/el 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

Also Published As

Publication number	Publication date
ATE458484T1 (de)	2010-03-15
PL1729775T3 (pl)	2011-03-31
US20080281101A1 (en)	2008-11-13
SI1958633T1 (sl)	2012-05-31
CA2561059A1 (en)	2005-10-06
WO2005092867A3 (en)	2005-11-10
CN101022807B (zh)	2012-05-09
GB0406757D0 (en)	2004-04-28
US8703945B2 (en)	2014-04-22
JP2007530521A (ja)	2007-11-01
CY1115040T1 (el)	2016-12-14
ES2379481T3 (es)	2012-04-26
CY1110091T1 (el)	2015-01-14
EP1958633A3 (de)	2008-08-27
KR20060130765A (ko)	2006-12-19
RS51306B (sr)	2010-12-31
EP1729775B1 (de)	2010-02-24
EP1958633B1 (de)	2011-12-14
JP5016478B2 (ja)	2012-09-05
SI1729775T1 (sl)	2010-07-30
IL178274A0 (en)	2006-12-31
PL1958633T3 (pl)	2012-12-31
ES2341658T3 (es)	2010-06-24
US20140316135A1 (en)	2014-10-23
WO2005092867A2 (en)	2005-10-06
AU2005225602A1 (en)	2005-10-06
DK1729775T3 (da)	2010-06-07
CN101022807A (zh)	2007-08-22
BRPI0507999A (pt)	2007-07-31
US9024025B2 (en)	2015-05-05
HRP20100287T1 (hr)	2010-07-31
CA2561059C (en)	2013-12-24
EP1958633A2 (de)	2008-08-20
PT1729775E (pt)	2010-05-27
DE602005019547D1 (de)	2010-04-08
PT1958633E (pt)	2012-03-27
DK1958633T3 (da)	2012-04-02
EP1729775A2 (de)	2006-12-13

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