EA200401533A1 - Способ получения росувастатина - Google Patents
Способ получения росувастатинаInfo
- Publication number
- EA200401533A1 EA200401533A1 EA200401533A EA200401533A EA200401533A1 EA 200401533 A1 EA200401533 A1 EA 200401533A1 EA 200401533 A EA200401533 A EA 200401533A EA 200401533 A EA200401533 A EA 200401533A EA 200401533 A1 EA200401533 A1 EA 200401533A1
- Authority
- EA
- Eurasian Patent Office
- Prior art keywords
- rosuvastatin
- obtaining
- obtaining rosuvastatin
- pyrimidinaldehyde
- pyrimidinecarboxaldehyde
- Prior art date
Links
- 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 abstract 2
- 229960000672 rosuvastatin Drugs 0.000 title abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 1
- 239000013067 intermediate product Substances 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- WZDZQGAQWAKGNY-UHFFFAOYSA-N n-[4-(2-fluorophenyl)-5-formyl-6-propan-2-ylpyrimidin-2-yl]-n-methylmethanesulfonamide Chemical compound CC(C)C1=NC(N(C)S(C)(=O)=O)=NC(C=2C(=CC=CC=2)F)=C1C=O WZDZQGAQWAKGNY-UHFFFAOYSA-N 0.000 abstract 1
- CCOXWRVWKFVFDG-UHFFFAOYSA-N pyrimidine-2-carbaldehyde Chemical compound O=CC1=NC=CC=N1 CCOXWRVWKFVFDG-UHFFFAOYSA-N 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
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
Настоящее изобретение относится к экономически эффективному и промышленно выгодному способу получения 4-4(фторфенил)-6-изопропил-2-(N-метил-N-метилсульфониламино)-5-пиримидинкарбоксальдегида, называемого здесь пиримидинальдегидом структурной формулы I, и к применению этого соединения в качестве промежуточного продукта при получении росувастатина.Отчет о международном поиске был опубликован 2004.05.21.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN575DE2002 | 2002-05-21 | ||
PCT/IB2003/001946 WO2003097614A2 (en) | 2002-05-21 | 2003-05-21 | Process for the preparation of rosuvastatin |
Publications (1)
Publication Number | Publication Date |
---|---|
EA200401533A1 true EA200401533A1 (ru) | 2005-06-30 |
Family
ID=29434392
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EA200401533A EA200401533A1 (ru) | 2002-05-21 | 2003-05-21 | Способ получения росувастатина |
Country Status (7)
Country | Link |
---|---|
US (1) | US20050222415A1 (ru) |
EP (1) | EP1585736A2 (ru) |
AR (1) | AR039836A1 (ru) |
AU (1) | AU2003228010A1 (ru) |
BR (1) | BR0311195A (ru) |
EA (1) | EA200401533A1 (ru) |
WO (1) | WO2003097614A2 (ru) |
Families Citing this family (56)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US7304156B2 (en) | 2001-07-13 | 2007-12-04 | Astrazeneca Uk Limited | Preparation of aminopyrimidine compounds |
GB0218781D0 (en) | 2002-08-13 | 2002-09-18 | Astrazeneca Ab | Chemical process |
GB0312896D0 (en) | 2003-06-05 | 2003-07-09 | Astrazeneca Ab | Chemical process |
WO2005021511A1 (en) * | 2003-08-27 | 2005-03-10 | Hetero Drugs Limited | A novel process for amorphous rosuvastatin calcium |
CA2537271A1 (en) | 2003-08-28 | 2005-03-17 | Teva Pharmaceutical Industries, Ltd. | Process for preparation of rosuvastatin calcium |
EP1816126A1 (en) * | 2003-08-28 | 2007-08-08 | Teva Pharmaceutical Industries Limited | Process for preparation of rosuvastatin calcium |
UY28501A1 (es) | 2003-09-10 | 2005-04-29 | Astrazeneca Uk Ltd | Compuestos químicos |
GB0324791D0 (en) | 2003-10-24 | 2003-11-26 | Astrazeneca Ab | Chemical process |
WO2005051921A1 (en) * | 2003-11-24 | 2005-06-09 | Teva Pharmaceutical Industries Ltd. | Crystalline ammonium salts of rosuvastatin |
PT1689723E (pt) | 2003-12-02 | 2011-07-06 | Teva Pharma | Padrão referência para a caracterização de rosuvastatina |
US7851624B2 (en) | 2003-12-24 | 2010-12-14 | Teva Pharamaceutical Industries Ltd. | Triol form of rosuvastatin and synthesis of rosuvastatin |
WO2006017357A1 (en) * | 2004-07-13 | 2006-02-16 | Teva Pharmaceutical Industries Ltd. | A process for the preparation of rosuvastatin involving a tempo-mediated oxidation step |
CZ298330B6 (cs) * | 2004-07-19 | 2007-08-29 | Zentiva, A. S. | Zpusob výroby 4-(4-fluorfenyl)-6-isopropyl-2-(N-methyl-N-methylsulfonylamino)-5-pyrimidinkarbaldehydu a jeho použití |
KR100622494B1 (ko) * | 2004-09-06 | 2006-09-19 | 현대자동차주식회사 | 조향 휠의 조립 구조 |
CN1763015B (zh) * | 2004-10-22 | 2011-06-22 | 四川抗菌素工业研究所有限公司 | 一种罗舒伐他汀及其药用盐的制备方法及中间体 |
CN100351240C (zh) * | 2005-01-19 | 2007-11-28 | 安徽省庆云医药化工有限公司 | 瑞舒伐他汀钙的合成方法 |
US20070037979A1 (en) * | 2005-02-22 | 2007-02-15 | Valerie Niddam-Hildesheim | Preparation of rosuvastatin |
US20070167625A1 (en) * | 2005-02-22 | 2007-07-19 | Anna Balanov | Preparation of rosuvastatin |
JP2008526781A (ja) * | 2005-02-22 | 2008-07-24 | 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 | ロスバスタチンの製造 |
KR101045895B1 (ko) * | 2005-02-22 | 2011-07-01 | 테바 파마슈티컬 인더스트리즈 리미티드 | 로수바스타틴의 제조 방법 |
US20090124803A1 (en) * | 2005-03-22 | 2009-05-14 | Pandurang Balwant Deshpande | Process for preparation of rosuvastatin |
EP1869005A1 (en) * | 2005-04-04 | 2007-12-26 | Unichem Laboratories Limited | Process for preparation of calcium salt of rosuvastatin |
EP1893585A1 (en) * | 2005-06-01 | 2008-03-05 | Fermion Oy | Process for the preparation of n-[4-(4-fluorophenyl)-5-formyl-6-isopropyl-pyrimidin-2-yl]-n-methylmethanesulfonamide |
JP5146965B2 (ja) * | 2005-06-24 | 2013-02-20 | レツク・フアーマシユーテイカルズ・デー・デー | 不純物を含まない非晶質ロスバスタチンカルシウムの調製方法 |
KR20090108671A (ko) * | 2005-08-16 | 2009-10-15 | 테바 파마슈티컬 인더스트리즈 리미티드 | 저염 함량의 로수바스타틴 칼슘 |
US7868169B2 (en) * | 2005-08-16 | 2011-01-11 | Teva Pharmaceutical Industries, Ltd. | Crystalline rosuvastatin intermediate |
CN100436428C (zh) * | 2005-08-22 | 2008-11-26 | 鲁南制药集团股份有限公司 | 瑞舒伐他汀及其盐的制备方法 |
JP2008526897A (ja) * | 2005-10-03 | 2008-07-24 | 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 | ロスバスタチンのジアステレオマー精製 |
WO2007074391A2 (en) * | 2005-12-28 | 2007-07-05 | Bakulesh Mafatlal Khamar | Preparation of a key intermediate in the synthesis of rosuvastatin |
ES2564250T3 (es) | 2006-05-03 | 2016-03-21 | Msn Laboratories Private Limited | Nuevo proceso para estatinas y sus sales farmacéuticamente aceptables de las mismas |
EP1948618A1 (en) * | 2006-09-18 | 2008-07-30 | Teva Pharmaceutical Industries Ltd. | Crystalline rosuvastatin calcium |
EP2086945B1 (en) | 2006-10-09 | 2016-01-06 | MSN Laboratories Private Limited | Novel process for the preparation of statins and their pharmaceutically acceptable salts thereof |
US8318933B2 (en) | 2006-10-31 | 2012-11-27 | Aurobindo Pharma Ltd | Process for preparing rosuvastatin calcium |
US8212034B2 (en) | 2006-12-13 | 2012-07-03 | Aurobindo Pharma Ltd. | Process for preparing rosuvastatin calcium |
WO2008093205A2 (en) * | 2007-01-31 | 2008-08-07 | Orchid Chemicals & Pharmaceuticals Limited | A method for the purification of rosuvastatin intermediate |
ES2385623T3 (es) | 2007-02-08 | 2012-07-27 | Aurobindo Pharma Limited | Un procedimiento mejorado para la preparación de rosuvastatina cálcica |
JP2009538831A (ja) | 2007-04-18 | 2009-11-12 | 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 | ロスバスタチン中間体及びロスバスタチンの調製方法。 |
CN101323597B (zh) * | 2007-06-11 | 2012-09-05 | 安徽省庆云医药化工有限公司 | 4-(4-氟苯基)-6-异丙基-2-(n-甲基-n-甲磺酰氨基)嘧啶-5-甲醛的制备方法 |
US20090069563A1 (en) | 2007-07-12 | 2009-03-12 | Valerie Niddam-Hildesheim | Rosuvastatin intermediates and their preparation |
EP2022784A1 (en) * | 2007-08-08 | 2009-02-11 | LEK Pharmaceuticals D.D. | Process for the preparation of methyl ester of rosuvastatin |
WO2009027081A2 (en) | 2007-08-28 | 2009-03-05 | Ratiopharm Gmbh | Process for preparing pentanoic diacid derivatives |
EP2298745B1 (en) | 2008-05-27 | 2014-09-03 | Changzhou Pharmaceutical Factory | Preparation method of rosuvastatin calcium and its intermediates |
US8394956B2 (en) * | 2008-09-30 | 2013-03-12 | Aurobindo Pharma Ltd. | Process for preparing pyrimidine propenaldehyde |
EP2752407B1 (en) | 2009-01-14 | 2015-09-23 | Krka Tovarna Zdravil, D.D., Novo Mesto | Crystalline rosuvastatin calcium trihydrate |
AU2010205464A1 (en) | 2009-01-15 | 2011-08-18 | Egis Gyogyszergyar Nyilvanosan Mukodo Reszvenytarsasag | Process for the preparation of rosuvastatin salts |
EP2387561A4 (en) | 2009-01-19 | 2012-07-25 | Msn Lab Ltd | IMPROVED PROCESS FOR THE PREPARATION OF HIGH-PURITY (3R, 5S) -7-β-CYCLOPROPYL-4- (4-FLUOROPHENYL) QUINOLIN-3-YL-3,5-DIHYDROXY-6 (E) -HEPTENOIC ACID, INCLUDING ITS PHARMACEUTICALLY ACCEPTABLE SALTS |
KR101160152B1 (ko) * | 2009-02-24 | 2012-06-27 | 한미사이언스 주식회사 | 스타틴 화합물 또는 그 염의 신규 제조방법, 및 이에 사용되는 중간체 화합물 |
EP2526099B1 (en) | 2010-01-18 | 2016-03-30 | MSN Laboratories Limited | Improved process for the preparation of amide intermediates and their use thereof |
WO2011141934A1 (en) | 2010-05-13 | 2011-11-17 | Matrix Laboratories Ltd. | An improved process for the preparation of an intermediate of hmg-coa reductase inhibitors |
WO2012011129A2 (en) * | 2010-07-22 | 2012-01-26 | Msn Laboratories Limited | Novel polymorph of bis[(e)-7-[4-(4-fluorophenyl)-6-iso-propyl-2-[methyl (methylsulfonyl)amino]pyrimidin-5-yl](3r,5s)-3,5-dihydroxyhept-6-enoic acid] calcium salt |
CN101955463B (zh) * | 2010-08-04 | 2012-01-04 | 重庆博腾制药科技股份有限公司 | 瑞舒伐他汀钙中间体的制备方法 |
HU230987B1 (hu) | 2010-11-29 | 2019-08-28 | Egis Gyógyszergyár Nyrt. | Eljárás nagy tisztaságú gyógyszeripari intermedierek előállítására |
AU2012345473B2 (en) | 2011-11-28 | 2017-05-25 | Mylan Laboratories Ltd | Process for producing chiral statin side chain intermediates employing candida|antarctica lipase B |
CN103134893B (zh) * | 2013-01-25 | 2014-12-03 | 峨眉山天梁星制药有限公司 | 一种3-叔丁基二甲硅氧基戊二酸酐的高效液相色谱分析法 |
CN111548312A (zh) * | 2020-06-01 | 2020-08-18 | 雅本化学股份有限公司 | 一种瑞舒伐他汀钙片及其制备工艺 |
CN113754590B (zh) * | 2021-09-06 | 2023-06-13 | 浙江乐普药业股份有限公司 | 一种瑞舒伐他汀钙中间体的制备方法 |
Family Cites Families (7)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US2698326A (en) * | 1954-12-28 | S-aminomethylpyrimtoines | ||
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 |
JP3400038B2 (ja) * | 1993-10-19 | 2003-04-28 | 塩野義製薬株式会社 | ピリミジン誘導体の製造方法 |
DE4338866C1 (de) * | 1993-11-13 | 1995-06-14 | Wolf Gmbh Richard | Medizinisches Instrument zur Applikation von Heißgas |
CZ298235B6 (cs) * | 1999-03-10 | 2007-08-01 | Lonza Ag | Zpusob výroby N-[5-(difenylfosfinoylmethyl)-4-(4-fluorfenyl)-6-isopropylpyrimidin-2-yl]-N-methylmethansulfonamidu |
GB0003305D0 (en) * | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
PL370407A1 (en) * | 2001-08-16 | 2005-05-30 | Teva Pharmaceutical Industries Ltd. | Processes for preparing calcium salt forms of statins |
-
2003
- 2003-05-21 WO PCT/IB2003/001946 patent/WO2003097614A2/en not_active Application Discontinuation
- 2003-05-21 EA EA200401533A patent/EA200401533A1/ru unknown
- 2003-05-21 AU AU2003228010A patent/AU2003228010A1/en not_active Abandoned
- 2003-05-21 AR ARP030101769A patent/AR039836A1/es unknown
- 2003-05-21 US US10/515,361 patent/US20050222415A1/en not_active Abandoned
- 2003-05-21 BR BR0311195-4A patent/BR0311195A/pt not_active IP Right Cessation
- 2003-05-21 EP EP03725478A patent/EP1585736A2/en not_active Withdrawn
Also Published As
Publication number | Publication date |
---|---|
BR0311195A (pt) | 2005-02-22 |
WO2003097614A2 (en) | 2003-11-27 |
WO2003097614A3 (en) | 2004-05-21 |
EP1585736A2 (en) | 2005-10-19 |
US20050222415A1 (en) | 2005-10-06 |
AR039836A1 (es) | 2005-03-02 |
AU2003228010A1 (en) | 2003-12-02 |
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