JP2009185041A5 - - Google Patents

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Publication number: JP2009185041A5
Authority: JP; Japan
Prior art keywords: formula; represented; producing; diol lactone; alkali metal
Prior art date: 2009-04-01
Legal status (The legal status 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 status listed.): Granted

Application number

JP2009089110A

Other languages

English (en)

Japanese (ja)

Other versions

JP5048709B2 (ja

JP2009185041A (ja

Filing date

2009-04-01

Publication date

2010-02-18

2009-04-01 Application filed filed Critical

2009-04-01 Priority to JP2009089110A priority Critical patent/JP5048709B2/ja

2009-04-01 Priority claimed from JP2009089110A external-priority patent/JP5048709B2/ja

2009-08-20 Publication of JP2009185041A publication Critical patent/JP2009185041A/ja

2010-02-18 Publication of JP2009185041A5 publication Critical patent/JP2009185041A5/ja

2012-10-17 Application granted granted Critical

2012-10-17 Publication of JP5048709B2 publication Critical patent/JP5048709B2/ja

2019-12-10 Anticipated expiration legal-status Critical

Status Expired - Fee Related legal-status Critical Current

Links

-1 diol lactone Chemical class 0.000 claims 6
238000004519 manufacturing process Methods 0.000 claims 4
WMFOQBRAJBCJND-UHFFFAOYSA-M Lithium hydroxide Chemical group [Li+].[OH-] WMFOQBRAJBCJND-UHFFFAOYSA-M 0.000 claims 3
KWYUFKZDYYNOTN-UHFFFAOYSA-M Potassium hydroxide Chemical compound [OH-].[K+] KWYUFKZDYYNOTN-UHFFFAOYSA-M 0.000 claims 3
HEMHJVSKTPXQMS-UHFFFAOYSA-M Sodium hydroxide Chemical compound [OH-].[Na+] HEMHJVSKTPXQMS-UHFFFAOYSA-M 0.000 claims 3
150000007529 inorganic bases Chemical class 0.000 claims 3
150000003333 secondary alcohols Chemical class 0.000 claims 3
150000003509 tertiary alcohols Chemical class 0.000 claims 3
KFZMGEQAYNKOFK-UHFFFAOYSA-N Isopropanol Chemical compound CC(C)O KFZMGEQAYNKOFK-UHFFFAOYSA-N 0.000 claims 2
PCZOHLXUXFIOCF-UHFFFAOYSA-N Monacolin X Natural products C12C(OC(=O)C(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 PCZOHLXUXFIOCF-UHFFFAOYSA-N 0.000 claims 2
DKGAVHZHDRPRBM-UHFFFAOYSA-N Tert-Butanol Chemical compound CC(C)(C)O DKGAVHZHDRPRBM-UHFFFAOYSA-N 0.000 claims 2
XSTXAVWGXDQKEL-UHFFFAOYSA-N Trichloroethylene Chemical compound ClC=C(Cl)Cl XSTXAVWGXDQKEL-UHFFFAOYSA-N 0.000 claims 2
239000002253 acid Substances 0.000 claims 2
150000008044 alkali metal hydroxides Chemical class 0.000 claims 2
PCZOHLXUXFIOCF-BXMDZJJMSA-N lovastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)[C@@H](C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 PCZOHLXUXFIOCF-BXMDZJJMSA-N 0.000 claims 2
229960004844 lovastatin Drugs 0.000 claims 2
QLJODMDSTUBWDW-UHFFFAOYSA-N lovastatin hydroxy acid Natural products C1=CC(C)C(CCC(O)CC(O)CC(O)=O)C2C(OC(=O)C(C)CC)CC(C)C=C21 QLJODMDSTUBWDW-UHFFFAOYSA-N 0.000 claims 2
238000000034 method Methods 0.000 claims 2
RYMZZMVNJRMUDD-UHFFFAOYSA-N SJ000286063 Natural products C12C(OC(=O)C(C)(C)CC)CC(C)C=C2C=CC(C)C1CCC1CC(O)CC(=O)O1 RYMZZMVNJRMUDD-UHFFFAOYSA-N 0.000 claims 1
229910052783 alkali metal Inorganic materials 0.000 claims 1
238000007273 lactonization reaction Methods 0.000 claims 1
RYMZZMVNJRMUDD-HGQWONQESA-N simvastatin Chemical compound C([C@H]1[C@@H](C)C=CC2=C[C@H](C)C[C@@H]([C@H]12)OC(=O)C(C)(C)CC)C[C@@H]1C[C@@H](O)CC(=O)O1 RYMZZMVNJRMUDD-HGQWONQESA-N 0.000 claims 1
229960002855 simvastatin Drugs 0.000 claims 1

JP2009089110A 1998-12-10 2009-04-01 シンバスタチンの製造方法 Expired - Fee Related JP5048709B2 (ja)

Priority Applications (1)

Application Number	Priority Date	Filing Date	Title
JP2009089110A JP5048709B2 (ja)	1998-12-10	2009-04-01	シンバスタチンの製造方法

Applications Claiming Priority (3)

Application Number	Priority Date	Filing Date	Title
JP1998351865		1998-12-10
JP35186598		1998-12-10
JP2009089110A JP5048709B2 (ja)	1998-12-10	2009-04-01	シンバスタチンの製造方法

Related Parent Applications (1)

Application Number	Title	Priority Date	Filing Date
JP2000586711A Division JP4440476B2 (ja)	1998-12-10	1999-12-10	シンバスタチンの製造方法

Publications (3)

Publication Number	Publication Date
JP2009185041A JP2009185041A (ja)	2009-08-20
JP2009185041A5 true JP2009185041A5 (2)	2010-02-18
JP5048709B2 JP5048709B2 (ja)	2012-10-17

Family

ID=18420148

Family Applications (2)

Application Number	Title	Priority Date	Filing Date
JP2000586711A Expired - Fee Related JP4440476B2 (ja)	1998-12-10	1999-12-10	シンバスタチンの製造方法
JP2009089110A Expired - Fee Related JP5048709B2 (ja)	1998-12-10	2009-04-01	シンバスタチンの製造方法

Family Applications Before (1)

Application Number	Title	Priority Date	Filing Date
JP2000586711A Expired - Fee Related JP4440476B2 (ja)	1998-12-10	1999-12-10	シンバスタチンの製造方法

Country Status (14)

Country	Link
US (1)	US6331641B1 (2)
EP (2)	EP1533308B1 (2)
JP (2)	JP4440476B2 (2)
KR (1)	KR100672269B1 (2)
CN (2)	CN1122029C (2)
AT (1)	ATE283849T1 (2)
AU (1)	AU1683000A (2)
CA (1)	CA2320163C (2)
CZ (2)	CZ299566B6 (2)
DE (1)	DE69922348T2 (2)
ES (1)	ES2234323T3 (2)
HU (1)	HUP0103021A3 (2)
SI (1)	SI20327B (2)
WO (1)	WO2000034264A1 (2)

Families Citing this family (26)

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Publication number	Priority date	Publication date	Assignee	Title
US6573385B1 (en)	1999-11-11	2003-06-03	Biocon India Limited	Process for manufacturing simvastatin and novel intermediates thereof
AU2127500A (en)	1999-11-11	2001-06-06	Biocon India Limited	Process for manufacturing simvastatin and the novel intermediates
GB0011120D0 (en) *	2000-05-09	2000-06-28	Avecia Ltd	Process
KR100361833B1 (ko) *	2000-06-20	2002-11-22	주식회사 엘지생명과학	심바스타틴의 제조방법
NL1015744C2 (nl) *	2000-07-19	2002-01-22	Dsm Nv	Werkwijze voor de bereiding van 2-(6-gesubstitueerde-1,3-dioxan-4-yl) azijnzuurderivaten.
MXPA04000322A (es) *	2001-07-13	2005-09-08	Astrazeneca Uk Ltd	Preparacion de compuestos de aminopirimidina.
KR100435142B1 (ko) *	2002-01-09	2004-06-09	한미약품 주식회사	개선된 심바스타틴의 제조방법
KR100502834B1 (ko) *	2002-03-25	2005-07-20	보령제약 주식회사	개선된 락톤화 반응에 의한 심바스타틴의 제조방법 및이의 정제방법
KR100502833B1 (ko) *	2002-03-25	2005-07-25	보령제약 주식회사	심바스타틴 및 이의 중간체 화합물들의 개선된 제조방법
US6603022B1 (en)	2002-05-10	2003-08-05	Biocon India Limited	Process for manufacturing Simvastatin and novel intermediates thereof
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
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
CN102703539A (zh) *	2003-10-21	2012-10-03	维莱尼姆公司	制备新伐他汀及中间体的方法
GB0324791D0 (en)	2003-10-24	2003-11-26	Astrazeneca Ab	Chemical process
WO2005058861A1 (en) *	2003-12-16	2005-06-30	Uk Chemipharm Co., Ltd.	Process for preparing simvastatin.
CN1754870A (zh) *	2004-09-30	2006-04-05	淮北市辉克药业有限公司	辛伐他汀的制备方法
GB0428328D0 (en) *	2004-12-24	2005-02-02	Astrazeneca Uk Ltd	Chemical process
GB0514078D0 (en) *	2005-07-08	2005-08-17	Astrazeneca Uk Ltd	Chemical process
US20110059493A1 (en) *	2007-08-27	2011-03-10	Brian Morgan	Methods for Making Simvastatin and Intermediates
JP2009114121A (ja) *	2007-11-06	2009-05-28	Kaneka Corp	シンバスタチンの製造方法
CN101575328B (zh) *	2008-05-09	2012-07-04	上海医药工业研究院	一种辛伐他汀中间体的合成方法
CN102690254B (zh) *	2008-05-09	2014-06-04	上海医药工业研究院	辛伐他汀铵盐中间体及其制备方法
CN110563680A (zh) *	2019-09-10	2019-12-13	山东罗欣药业集团恒欣药业有限公司	一种治疗高脂血症药物的制备方法
CN110483459A (zh) *	2019-09-10	2019-11-22	山东罗欣药业集团恒欣药业有限公司	一种辛伐他汀的合成方法

Family Cites Families (18)

* Cited by examiner, † Cited by third party
Publication number	Priority date	Publication date	Assignee	Title
US4444784A (en) *	1980-08-05	1984-04-24	Merck & Co., Inc.	Antihypercholesterolemic compounds
ZA81703B (en) *	1980-02-04	1982-09-29	Merck & Co Inc	New antihypercholesterolemic compounds,intermediates and processes
JPS58188872A (ja) *	1982-04-26	1983-11-04	Suntory Ltd	オクタヒドロナフタレン誘導体及びその製造法
US4837205A (en) *	1986-09-02	1989-06-06	Merck & Co., Inc.	Prodrugs of antihypercholesterolemic compounds
US4916239A (en) *	1988-07-19	1990-04-10	Merck & Co., Inc.	Process for the lactonization of mevinic acids and analogs thereof
GB8915280D0 (en) *	1989-07-04	1989-08-23	British Bio Technology	Compounds
US5072002A (en) *	1989-07-18	1991-12-10	The Governors Of The University Of Alberta	Synthesis of cholesterol-lowering agents
US5093363A (en) *	1989-08-22	1992-03-03	Shionogi & Co., Ltd.	2,4,6-substituted phenol derivatives
EP0415488B1 (en) *	1989-08-31	1994-04-20	Merck & Co. Inc.	7-Substituted HMG-COA reductase inhibitors
US5393893A (en) *	1993-11-08	1995-02-28	Apotex, Inc.	Process for producing simvastatin and analogs thereof
EA000954B1 (ru) *	1995-12-06	2000-08-28	Балканфарма - Разград Ад	Способ получения ловастатина
US5763653A (en) *	1997-03-13	1998-06-09	Ranbaxy Laboratories, Ltd.	Key intermediates in the manufacture of simvastatin
CA2185961A1 (en) *	1996-09-19	1998-03-20	K.S. Keshava Murthy	Process for producing simvastatin
US5763646A (en) *	1997-03-13	1998-06-09	Ranbaxy Laboratories, Ltd.	Process for manufacturing simvastatin from lovastatin or mevinolinic acid
SI9700202A (sl) *	1997-01-24	1998-08-31	Ranbaxy Laboratories Limited	Postopek izdelave simvastatina iz lovastatina ali mevinolinske kisline
ES2266671T3 (es) *	1997-01-28	2007-03-01	Plus Chemicals B.V.	Proceso para la produccion de estatinas semisinteticas a traves de nuevos intermediarios.
SI9800057A (sl) *	1998-02-26	1999-08-31	Krka, Tovarna Zdravil, D.D.	Postopek za pripravo simvastatina in njegovih derivatov
EP0940395A1 (en) *	1998-03-05	1999-09-08	Synthon B.V.	Process for producing simvastatin and/or its derivatives

1999
- 1999-12-10 CN CN99802754A patent/CN1122029C/zh not_active Expired - Fee Related
- 1999-12-10 KR KR1020007008648A patent/KR100672269B1/ko not_active Expired - Fee Related
- 1999-12-10 ES ES99959738T patent/ES2234323T3/es not_active Expired - Lifetime
- 1999-12-10 AT AT99959738T patent/ATE283849T1/de not_active IP Right Cessation
- 1999-12-10 SI SI9920024A patent/SI20327B/sl active Search and Examination
- 1999-12-10 EP EP04023298.5A patent/EP1533308B1/en not_active Expired - Lifetime
- 1999-12-10 DE DE69922348T patent/DE69922348T2/de not_active Expired - Lifetime
- 1999-12-10 JP JP2000586711A patent/JP4440476B2/ja not_active Expired - Fee Related
- 1999-12-10 CZ CZ20080099A patent/CZ299566B6/cs not_active IP Right Cessation
- 1999-12-10 EP EP99959738A patent/EP1055671B1/en not_active Expired - Lifetime
- 1999-12-10 AU AU16830/00A patent/AU1683000A/en not_active Abandoned
- 1999-12-10 CZ CZ20003149A patent/CZ299522B6/cs not_active IP Right Cessation
- 1999-12-10 US US09/601,794 patent/US6331641B1/en not_active Expired - Lifetime
- 1999-12-10 WO PCT/JP1999/006929 patent/WO2000034264A1/ja not_active Ceased
- 1999-12-10 CN CNB031530451A patent/CN1226296C/zh not_active Expired - Fee Related
- 1999-12-10 HU HU0103021A patent/HUP0103021A3/hu unknown
- 1999-12-10 CA CA002320163A patent/CA2320163C/en not_active Expired - Fee Related
2009
- 2009-04-01 JP JP2009089110A patent/JP5048709B2/ja not_active Expired - Fee Related

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