AR039836A1 - Proceso para la preparacion de un aldehido de pirimidina util para la preparacion de rosuvastatina - Google Patents
Proceso para la preparacion de un aldehido de pirimidina util para la preparacion de rosuvastatinaInfo
- Publication number
- AR039836A1 AR039836A1 ARP030101769A ARP030101769A AR039836A1 AR 039836 A1 AR039836 A1 AR 039836A1 AR P030101769 A ARP030101769 A AR P030101769A AR P030101769 A ARP030101769 A AR P030101769A AR 039836 A1 AR039836 A1 AR 039836A1
- Authority
- AR
- Argentina
- Prior art keywords
- structural formula
- derivative
- preparation
- pyrimidine
- compound
- Prior art date
Links
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)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La rosuvastatina es útil como antihipercolesterolémico. Reivindicación 1: Un proceso para la preparación de 4-(4-fluorofenil)-6-isopropil-2-(N-metil-N-metilsulfonilamino)pirimidina-5-il-carboxaldehido de la fórmula estructural (1) que comprende: a) la condensación de 4-fluorobenzaldehido de la fórmula estructural (2) con un compuesto de la fórmula estructural (3), en donde R1 es independientemente alquilo C2-6, cicloalquilo C1-6 o aralquilo, para obtener una olefina de la fórmula estructural (4); b) la reacción de la olefina con isotiourea de la fórmula estructural (5), en donde R2 es independientemente alquilo C2-6, cicloalquilo C1-6, o aralquilo, para obtener un derivado dihidropirimidínico cíclico de la fórmula estructural (6); c) la aromatización del derivado de dihidropirimidina con dióxido de manganeso-g para obtener un compuesto de pirimidina de la fórmula estructural (7); d) la oxidación del compuesto de pirimidina para obtener un derivado sulfonilo de la fórmula estructural (8); e) la reacción del derivado de sulfonilo con metilamina para obtener un derivado de N-metilpirimidina de la fórmula estructural (9); f) la reacción del derivado de N-metilo pirimidina con cloruro de metanosulfonilo para obtener un derivado de N-metilo metanosulfonamida de la fórmula estructural (10); g) la reducción del derivado de N-metilo metanosulfonamida con hidruro de diisobutilaluminio (DIBAL) en tolueno para obtener un compuesto alcohólico de la fórmula estructural (11); y h) la oxidación del compuesto alcohólico para obtener un aldehido de pirimidina de la fórmula estructural (1).
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN575DE2002 | 2002-05-21 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR039836A1 true AR039836A1 (es) | 2005-03-02 |
Family
ID=29434392
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP030101769A AR039836A1 (es) | 2002-05-21 | 2003-05-21 | Proceso para la preparacion de un aldehido de pirimidina util para la preparacion de rosuvastatina |
Country Status (7)
Country | Link |
---|---|
US (1) | US20050222415A1 (es) |
EP (1) | EP1585736A2 (es) |
AR (1) | AR039836A1 (es) |
AU (1) | AU2003228010A1 (es) |
BR (1) | BR0311195A (es) |
EA (1) | EA200401533A1 (es) |
WO (1) | WO2003097614A2 (es) |
Families Citing this family (56)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
AU2002318041B2 (en) | 2001-07-13 | 2008-01-03 | 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 |
WO2005023778A2 (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 |
CA2546701C (en) * | 2003-11-24 | 2010-07-27 | Teva Pharmaceutical Industries Ltd. | Crystalline ammonium salts of rosuvastatin |
CN1894221B (zh) * | 2003-12-02 | 2012-08-08 | 特瓦制药工业有限公司 | 用于表征罗苏伐他汀的参照标准品 |
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 |
US20070167625A1 (en) * | 2005-02-22 | 2007-07-19 | Anna Balanov | Preparation of rosuvastatin |
CN101119975A (zh) * | 2005-02-22 | 2008-02-06 | 特瓦制药工业有限公司 | 罗舒伐他汀的制备 |
US20070037979A1 (en) * | 2005-02-22 | 2007-02-15 | Valerie Niddam-Hildesheim | Preparation of rosuvastatin |
WO2006091771A2 (en) * | 2005-02-22 | 2006-08-31 | Teva Pharmaceutical Industries Ltd. | Preparation of rosuvastatin |
EP1863773A1 (en) * | 2005-03-22 | 2007-12-12 | Unichem Laboratories Limited | Process for preparation of rosuvastatin |
US20080161560A1 (en) * | 2005-04-04 | 2008-07-03 | Pandurang Balwant Deshpande | Process for Preparation of Calcium Salt of Rosuvastatin |
WO2006128954A1 (en) * | 2005-06-01 | 2006-12-07 | Fermion Oy | Process for the preparation of n-[4-(4-fluorophenyl)-5-formyl-6-isopropyl-pyrimidin-2-yl]-n-methylmethanesulfonamide |
AU2006261087B2 (en) * | 2005-06-24 | 2010-09-30 | Lek Pharmaceuticals D.D. | Process for preparing amorphous rosuvastatin calcium free of impurities |
BRPI0605917A2 (pt) * | 2005-08-16 | 2009-05-26 | Teva Pharma | intermediário cristalino de rosuvastatina |
KR20090108671A (ko) * | 2005-08-16 | 2009-10-15 | 테바 파마슈티컬 인더스트리즈 리미티드 | 저염 함량의 로수바스타틴 칼슘 |
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 |
BRPI0606170A2 (pt) * | 2005-10-03 | 2009-06-02 | Teva Pharma Ltd | purificação diastereomérica de rosuvastatina |
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 |
WO2008036286A1 (en) * | 2006-09-18 | 2008-03-27 | 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 |
EP2079712A2 (en) | 2006-10-31 | 2009-07-22 | Aurobindo Pharma Limited | An improved process for preparing rosuvastatin calcium |
WO2008072078A1 (en) * | 2006-12-13 | 2008-06-19 | Aurobindo Pharma Limited | An improved process for preparing rosuvastatin caclium |
WO2008093205A2 (en) * | 2007-01-31 | 2008-08-07 | Orchid Chemicals & Pharmaceuticals Limited | A method for the purification of rosuvastatin intermediate |
CA2677809A1 (en) | 2007-02-08 | 2008-08-14 | Aurobindo Pharma Limited | An improved process for preparation of rosuvastatin calcium |
KR20090018964A (ko) | 2007-04-18 | 2009-02-24 | 테바 파마슈티컬 인더스트리즈 리미티드 | Hmg-coa 환원 효소 억제제의 중간체의 제조 방법 |
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 |
US7884226B2 (en) | 2007-07-12 | 2011-02-08 | Teva Pharmaceutical Industries, Ltd. | Purification of rosuvatatin intermediate by thin film evaporation and chemical method |
EP2022784A1 (en) * | 2007-08-08 | 2009-02-11 | LEK Pharmaceuticals D.D. | Process for the preparation of methyl ester of rosuvastatin |
US20110065920A1 (en) | 2007-08-28 | 2011-03-17 | Ratiopharm Gmbh | Process for preparing pentanoic diacid derivatives |
CA2725052C (en) | 2008-05-27 | 2014-09-16 | Changzhou Pharmaceutical Factory Co., Ltd. | Preparation method of rosuvastatin calcium and its intermediates |
US8394956B2 (en) * | 2008-09-30 | 2013-03-12 | Aurobindo Pharma Ltd. | Process for preparing pyrimidine propenaldehyde |
WO2010081861A1 (en) | 2009-01-14 | 2010-07-22 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Process for the preparation of rosuvastatin |
BRPI1005147A2 (pt) | 2009-01-15 | 2019-09-24 | Egis Gyogyszergyar Nyilvanosan Muekoedoe Reszvenytarsasag | processo de preparação de sais de rosuvastatina |
US8487105B2 (en) | 2009-01-19 | 2013-07-16 | Msn Laboratories Limited | Process for preparing pitavastatin, intermediates and pharmaceuctically acceptable salts thereof |
KR101160152B1 (ko) * | 2009-02-24 | 2012-06-27 | 한미사이언스 주식회사 | 스타틴 화합물 또는 그 염의 신규 제조방법, 및 이에 사용되는 중간체 화합물 |
WO2011086584A2 (en) | 2010-01-18 | 2011-07-21 | 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 |
CN104066846B (zh) | 2011-11-28 | 2018-09-25 | 迈兰实验室有限公司 | 采用南极假丝酵母脂肪酶b制备手性他汀侧链中间体的方法 |
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 |
SK284027B6 (sk) * | 1999-03-10 | 2004-08-03 | Lonza Ag | Spôsob výroby N-[5-(difenylfosfinoylmetyl)-4-(4-fluórfenyl)-6- izopropylpyrimidin-2-yl]-N-metylmetánsulfónamidu |
GB0003305D0 (en) * | 2000-02-15 | 2000-04-05 | Zeneca Ltd | Pyrimidine derivatives |
MXPA04001451A (es) * | 2001-08-16 | 2005-02-17 | Teva Pharma | Procesos para preparar formas de sal de calcio de estatinas. |
-
2003
- 2003-05-21 WO PCT/IB2003/001946 patent/WO2003097614A2/en not_active Application Discontinuation
- 2003-05-21 EP EP03725478A patent/EP1585736A2/en not_active Withdrawn
- 2003-05-21 BR BR0311195-4A patent/BR0311195A/pt not_active IP Right Cessation
- 2003-05-21 US US10/515,361 patent/US20050222415A1/en not_active Abandoned
- 2003-05-21 EA EA200401533A patent/EA200401533A1/ru unknown
- 2003-05-21 AR ARP030101769A patent/AR039836A1/es unknown
- 2003-05-21 AU AU2003228010A patent/AU2003228010A1/en not_active Abandoned
Also Published As
Publication number | Publication date |
---|---|
WO2003097614A3 (en) | 2004-05-21 |
EA200401533A1 (ru) | 2005-06-30 |
EP1585736A2 (en) | 2005-10-19 |
AU2003228010A1 (en) | 2003-12-02 |
WO2003097614A2 (en) | 2003-11-27 |
BR0311195A (pt) | 2005-02-22 |
US20050222415A1 (en) | 2005-10-06 |
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