ES2166932T3 - Productos intermediarios clave para la preparacion de simvastatina. - Google Patents
Productos intermediarios clave para la preparacion de simvastatina.Info
- Publication number
- ES2166932T3 ES2166932T3 ES97107059T ES97107059T ES2166932T3 ES 2166932 T3 ES2166932 T3 ES 2166932T3 ES 97107059 T ES97107059 T ES 97107059T ES 97107059 T ES97107059 T ES 97107059T ES 2166932 T3 ES2166932 T3 ES 2166932T3
- Authority
- ES
- Spain
- Prior art keywords
- simvastatin
- ring
- preparation
- intermediate products
- open
- Prior art date
- 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.)
- Expired - Lifetime
Links
- 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 title abstract 4
- 229960002855 simvastatin Drugs 0.000 title abstract 4
- 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 title abstract 4
- 239000013067 intermediate product Substances 0.000 title 1
- 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 abstract 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 abstract 2
- 239000007858 starting material Substances 0.000 abstract 2
- HTJDQJBWANPRPF-UHFFFAOYSA-N Cyclopropylamine Chemical compound NC1CC1 HTJDQJBWANPRPF-UHFFFAOYSA-N 0.000 abstract 1
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical class [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 abstract 1
- HWDVTQAXQJQROO-UHFFFAOYSA-N cyclopropylazanide Chemical compound [NH-]C1CC1 HWDVTQAXQJQROO-UHFFFAOYSA-N 0.000 abstract 1
- BHIWKHZACMWKOJ-UHFFFAOYSA-N isobutyric acid methyl ester Natural products COC(=O)C(C)C BHIWKHZACMWKOJ-UHFFFAOYSA-N 0.000 abstract 1
- 229960004844 lovastatin Drugs 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- QLJODMDSTUBWDW-BXMDZJJMSA-N mevinolinic acid Chemical compound C1=C[C@H](C)[C@H](CC[C@@H](O)C[C@@H](O)CC(O)=O)[C@H]2[C@@H](OC(=O)[C@@H](C)CC)C[C@@H](C)C=C21 QLJODMDSTUBWDW-BXMDZJJMSA-N 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
- C07C235/02—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton
- C07C235/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups bound to acyclic carbon atoms and singly-bound oxygen atoms bound to the same carbon skeleton the carbon skeleton being unsaturated and containing rings other than six-membered aromatic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2601/00—Systems containing only non-condensed rings
- C07C2601/02—Systems containing only non-condensed rings with a three-membered ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
- C07C2602/00—Systems containing two condensed rings
- C07C2602/02—Systems containing two condensed rings the rings having only two atoms in common
- C07C2602/14—All rings being cycloaliphatic
- C07C2602/26—All rings being cycloaliphatic the ring system containing ten carbon atoms
- C07C2602/28—Hydrogenated naphthalenes
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Pyrane Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
UN PROCESO PARA PREPARAR SIMVASTATINA A PARTIR DE LOVASTATINA O ACIDO MEVINOLINICO EN SU FORMA DE SAL INCLUYE TRATAR CUALQUIERA DE LOS MATERIALES DE PARTIDA CON CICLOPROPILO O BUTILAMIDA, ABRIENDOSE DE ESE MODO EL ANILLO PIRANONA CUANDO EL MATERIAL DE PARTIDA ES LOVASTATINA, AÑADIR UN GRUPO METILO A LA CADENA LATERAL 2 - METILBUTIRATO, Y POSTERIORMENTE CERRAR EL ANILLO PIRANONA ABIERTO PARA PRODUCIR SIMVASTATINA. EL PROCESO SE REALIZA SIN PROTEGER Y DESPROTEGER LOS DOS GRUPOS HIDROXI DEL ANILLO PIRANONA ABIERTO. EN UNA REALIZACION PREFERIDA, SE TRATA EL MATERIAL DE PARTIDA CON CICLOPROPILAMINA, LO CUAL PRODUCE SIMVASTATINA VIA EL NUEVO INTERMEDIO CICLOPROPILAMIDA DE LOVASTATINA.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US08/816,574 US5763653A (en) | 1997-03-13 | 1997-03-13 | Key intermediates in the manufacture of simvastatin |
Publications (1)
Publication Number | Publication Date |
---|---|
ES2166932T3 true ES2166932T3 (es) | 2002-05-01 |
Family
ID=25221008
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ES97107059T Expired - Lifetime ES2166932T3 (es) | 1997-03-13 | 1997-04-29 | Productos intermediarios clave para la preparacion de simvastatina. |
Country Status (9)
Country | Link |
---|---|
US (1) | US5763653A (es) |
EP (1) | EP0864560B1 (es) |
AT (1) | ATE209627T1 (es) |
CZ (1) | CZ286576B6 (es) |
DE (1) | DE69708591T2 (es) |
ES (1) | ES2166932T3 (es) |
SI (1) | SI9700203A (es) |
SK (1) | SK282909B6 (es) |
ZA (1) | ZA974022B (es) |
Families Citing this family (20)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP0940395A1 (en) * | 1998-03-05 | 1999-09-08 | Synthon B.V. | Process for producing simvastatin and/or its derivatives |
SI20070A (sl) * | 1998-09-18 | 2000-04-30 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Nove soli inhibitorjev HMG-CoA reduktaze |
CN1226296C (zh) * | 1998-12-10 | 2005-11-09 | 钟渊化学工业株式会社 | 制备辛伐他汀的方法 |
CO5140104A1 (es) * | 1999-02-16 | 2002-03-22 | Novartis Ag | Derivados de mevinolina y preparacion farmaceuticas que los contienen |
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 |
AU2001228796A1 (en) * | 2000-09-13 | 2002-04-02 | Biocon India Limited | Process for manufacturing simvastatin and the novel intermediates |
KR100502833B1 (ko) * | 2002-03-25 | 2005-07-25 | 보령제약 주식회사 | 심바스타틴 및 이의 중간체 화합물들의 개선된 제조방법 |
SI21187A (sl) | 2002-03-26 | 2003-10-31 | Krka, Tovarna Zdravil D.D., Novo Mesto | Postopek za pripravo 4-oksitetrahidropiran-2-onov |
US6603022B1 (en) | 2002-05-10 | 2003-08-05 | Biocon India Limited | Process for manufacturing Simvastatin and novel intermediates thereof |
US20080293750A1 (en) * | 2002-10-17 | 2008-11-27 | Anna Helgadottir | Susceptibility Gene for Myocardial Infarction, Stroke, Paod and Methods of Treatment |
US20060019269A1 (en) * | 2002-10-17 | 2006-01-26 | Decode Genetics, Inc. | Susceptibility gene for myocardial infarction, stroke, and PAOD, methods of treatment |
US6995277B2 (en) | 2003-02-11 | 2006-02-07 | Plus Chemicals, B.V. | Process for preparing simvastatin having controlled ranges of simvastatin dimer content |
KR20040092790A (ko) * | 2003-04-29 | 2004-11-04 | 씨제이 주식회사 | 심바스타틴 중간체 제조방법 |
US8158362B2 (en) * | 2005-03-30 | 2012-04-17 | Decode Genetics Ehf. | Methods of diagnosing susceptibility to myocardial infarction and screening for an LTA4H haplotype |
US20100216863A1 (en) * | 2004-01-30 | 2010-08-26 | Decode Genetics Ehf. | Susceptibility Gene for Myocardial Infarction, Stroke, and PAOD; Methods of Treatment |
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 |
WO2007020079A2 (en) * | 2005-08-17 | 2007-02-22 | Synthon B.V. | Orally disintegratable simvastatin tablets |
ES2524725T3 (es) | 2009-09-30 | 2014-12-11 | Codexis, Inc. | Polipéptidos LovD variantes y sus usos. |
SG10201504099WA (en) | 2009-10-08 | 2015-06-29 | Univ California | LovD MUTANTS EXHIBITING IMPROVED PROPERTIES TOWARDS SIMVASTATIN SYNTHESIS |
Family Cites Families (13)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
JPS5612114B2 (es) * | 1974-06-07 | 1981-03-18 | ||
US4231938A (en) * | 1979-06-15 | 1980-11-04 | Merck & Co., Inc. | Hypocholesteremic fermentation products and process of preparation |
US4444784A (en) * | 1980-08-05 | 1984-04-24 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
US4293496A (en) * | 1980-02-04 | 1981-10-06 | Merck & Co., Inc. | 6(R)-[2-(8-Hydroxy-2,6-dimethylpolyhydronaphthyl-1)-ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-ones |
US4450171A (en) * | 1980-08-05 | 1984-05-22 | Merck & Co., Inc. | Antihypercholesterolemic compounds |
US4584389A (en) * | 1983-10-11 | 1986-04-22 | Merck & Co., Inc. | Processes for preparing 6(R)-[2-[8(S)(2,2-dimethylbutyryloxy)-2(S),6(S)-dimethyl-1,2,3,4,4a(S),5,6,7,8,8a(S)-decahydronaphthyl-1(S)]ethyl]-4(R)-hydroxy-3,4,5,6-tetrahydro-2H-pyran-2-one |
US4582915A (en) * | 1983-10-11 | 1986-04-15 | Merck & Co., Inc. | Process for C-methylation of 2-methylbutyrates |
US4611081A (en) * | 1985-07-05 | 1986-09-09 | Merck & Co., Inc. | Process for the preparation of HMG-CoA reductase inhibitors intermediates |
US4820850A (en) * | 1987-07-10 | 1989-04-11 | Merck & Co., Inc. | Process for α-C-alkylation of the 8-acyl group on mevinolin and analogs thereof |
US4908452A (en) * | 1987-12-21 | 1990-03-13 | Merck & Co., Inc. | Process for preparing nitriles |
US5223415A (en) * | 1990-10-15 | 1993-06-29 | Merck & Co., Inc. | Biosynthetic production of 7-[1',2',6',7',8',8a'(R)-hexahydro-2'(S),6'(R)-dimethyl-8'(S)-hydroxy-1'(S)-naphthyl]-3(R),5(R)-dihydroxyheptanoic acid (triol acid) |
US5159104A (en) * | 1991-05-01 | 1992-10-27 | Merck & Co., Inc. | Process to simvastatin ester |
US5393893A (en) * | 1993-11-08 | 1995-02-28 | Apotex, Inc. | Process for producing simvastatin and analogs thereof |
-
1997
- 1997-03-13 US US08/816,574 patent/US5763653A/en not_active Expired - Lifetime
- 1997-04-29 ES ES97107059T patent/ES2166932T3/es not_active Expired - Lifetime
- 1997-04-29 AT AT97107059T patent/ATE209627T1/de not_active IP Right Cessation
- 1997-04-29 EP EP97107059A patent/EP0864560B1/en not_active Expired - Lifetime
- 1997-04-29 DE DE69708591T patent/DE69708591T2/de not_active Expired - Fee Related
- 1997-05-30 ZA ZA9704022A patent/ZA974022B/xx unknown
- 1997-07-29 SI SI9700203A patent/SI9700203A/sl not_active IP Right Cessation
- 1997-08-20 CZ CZ19972650A patent/CZ286576B6/cs not_active IP Right Cessation
- 1997-08-25 SK SK1165-97A patent/SK282909B6/sk unknown
Also Published As
Publication number | Publication date |
---|---|
SK282909B6 (sk) | 2003-01-09 |
SK116597A3 (en) | 1999-05-07 |
EP0864560A1 (en) | 1998-09-16 |
ZA974022B (en) | 1997-12-09 |
US5763653A (en) | 1998-06-09 |
CZ265097A3 (cs) | 1998-09-16 |
SI9700203A (sl) | 1998-10-31 |
CZ286576B6 (cs) | 2000-05-17 |
EP0864560B1 (en) | 2001-11-28 |
DE69708591T2 (de) | 2002-08-01 |
DE69708591D1 (de) | 2002-01-10 |
ATE209627T1 (de) | 2001-12-15 |
Similar Documents
Publication | Publication Date | Title |
---|---|---|
ES2166932T3 (es) | Productos intermediarios clave para la preparacion de simvastatina. | |
DE69534130D1 (de) | Verbindungen zur behandlung von erkrankungen,die mit des vasculogenese und/oder angiogenese in verbunden stehen. | |
DE69729587D1 (de) | Behandlung von migränekopfschmerzen mit metoclopramid und einem nsaid | |
ATE515513T1 (de) | Behandlung von fibrose durch antagonismus zwischen il-13 und il-13-rezeptorketten | |
DE60013827D1 (de) | Vorrichtung zum behandeln von schlachtprodukten | |
BR0207760A (pt) | Composição farmacêutica, uso da mesma, métodos para o tratamento de dor e de inflamação, e, processo para a preparação de uma composição | |
DE69925256D1 (de) | Trisubstituierte 1,3,5-triazine derivate zur behandlung von hiv infektionen | |
ATE403437T1 (de) | Lfa-1 antagonisten und tnf-alpha antagonisten zur behandlung von rheumatoiden arthritis | |
DE60043308D1 (de) | Verfahren zur behandlung der schädigung des zentralnervensystems durch ischämie oder durch hämorrhagie mit antagonisten von alpha4 integrin | |
DE602004003587D1 (de) | Kosmetische verwendung einer zusammensetzung mit mindestens einem oxazolin als wirkstoff, als abnehmprodukt und/oder zur prävention und/oder behandlung von cellulite | |
WO2004016256A3 (en) | AGONISM OF THE 5HT2a RECEPTOR FOR TREATMENT OF THERMOREGULATORY DYSFUNCTION | |
BR9305083A (pt) | Dispositivo de transporte para máquinas, para o tratamento de garrafas ou recipientes semelhantes | |
PT942815E (pt) | Metodo de utilizacao de materiais compositos lenhocelulosicos reciclados | |
DE50208897D1 (de) | Vorrichtung zum abschwarten und enthäuten von behandlungsgut | |
BR9813666A (pt) | Processos para preparar uma composição farmacêutica e para tratamento de pacientes, e, composição farmacêutica | |
IL153557A0 (en) | Antibodies and antagonists to antimicrobial peptides for the purpose of treating, inhibiting and preventing auto immune diseases | |
AR110470A1 (es) | Terapia de combinación para tratar la enfermedad de alzheimer | |
DE69121598T2 (de) | Verfahren, um das Verpacken von sterilisiertem Mineralwasser vorzubereiten sowie verpacktes, sterilisiertes Mineralwasser | |
EA200100785A1 (ru) | Шипучие слабительные средства | |
MXPA05004121A (es) | Metodos para tratar la enfermedad de ojo reseco con lantibioticos. | |
Luszczki et al. | Effect of N-(m-bromoanilinomethyl)-p-isopropoxyphenylsuccinimide on the anticonvulsant action of four classical antiepileptic drugs in the mouse maximal electroshock-induced seizure model | |
DE50015379D1 (de) | Vorrichtung zur Überkopf-Behandlung von Flaschen oder dergleichen Behältern | |
TW200509882A (en) | Beauty method | |
DE69910332D1 (de) | Sicherheitsvorrichtung, insbesondere zum Schutz von Bereichen | |
DE69403197D1 (de) | Die verwendung von anti-helminth impfstoffen zur kontrolle von parasitären krankheiten, die mit einem verlust der natürlichen immunität assoziiert sind |