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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 rosuvastatina

Info

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
Application number
ARP030101769A
Other languages
English (en)
Inventor
Yatendra Kumar
Shantanu De
Mohammad Rafeeq
Hashim Nizar Poovanathi Meeran
Swargam Sathyanarayana
Original Assignee
Ranbaxy Lab 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.)
Filing date
Publication date
Application filed by Ranbaxy Lab Ltd filed Critical Ranbaxy Lab Ltd
Publication of AR039836A1 publication Critical patent/AR039836A1/es

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)
  • Plural Heterocyclic Compounds (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic 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).
ARP030101769A 2002-05-21 2003-05-21 Proceso para la preparacion de un aldehido de pirimidina util para la preparacion de rosuvastatina AR039836A1 (es)

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)

* 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
AU2003269478A1 (en) * 2003-08-27 2005-03-16 Hetero Drugs Limited A novel process for amorphous rosuvastatin calcium
EP1562912A2 (en) * 2003-08-28 2005-08-17 Teva Pharmaceutical Industries Limited 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
US7244844B2 (en) 2003-12-02 2007-07-17 Teva Pharmaceutical Industries Ltd. Reference standard for characterization of rosuvastatin
US7851624B2 (en) 2003-12-24 2010-12-14 Teva Pharamaceutical Industries Ltd. Triol form of rosuvastatin and synthesis of rosuvastatin
CA2573857A1 (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
CN101128437A (zh) * 2005-02-22 2008-02-20 特瓦制药工业有限公司 不含罗苏伐他汀烷基醚的罗苏伐他汀及其盐以及制备它们的方法
JP4713574B2 (ja) 2005-02-22 2011-06-29 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 ロスバスタチンアルキルエーテルを含まないロスバスタチンおよびその塩およびそれらを製造する方法
US20070037979A1 (en) * 2005-02-22 2007-02-15 Valerie Niddam-Hildesheim Preparation of rosuvastatin
EP1863773A1 (en) * 2005-03-22 2007-12-12 Unichem Laboratories Limited Process for preparation of rosuvastatin
EP1869005A1 (en) * 2005-04-04 2007-12-26 Unichem Laboratories Limited 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
EP2508514B1 (en) 2005-06-24 2017-10-18 LEK Pharmaceuticals d.d. Process for preparing amorphous rosuvastatin calcium free of impurities
KR20090108671A (ko) * 2005-08-16 2009-10-15 테바 파마슈티컬 인더스트리즈 리미티드 저염 함량의 로수바스타틴 칼슘
CA2619576C (en) * 2005-08-16 2011-12-06 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
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
HUE027872T2 (en) 2006-05-03 2016-11-28 Msn Laboratories Private Ltd A novel process for statins and their pharmaceutically acceptable salts
WO2008036286A1 (en) * 2006-09-18 2008-03-27 Teva Pharmaceutical Industries Ltd. Crystalline rosuvastatin calcium
ES2567171T3 (es) 2006-10-09 2016-04-20 Msn Laboratories Private Limited Nuevo procedimiento para la preparación de estatinas y sus sales farmacéuticamente aceptables
WO2008053334A2 (en) 2006-10-31 2008-05-08 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
AU2008212622B2 (en) 2007-02-08 2011-01-27 Aurobindo Pharma Limited An improved process for preparation of rosuvastatin calcium
JP2009531466A (ja) 2007-04-18 2009-09-03 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 ＨＭＧ−ＣｏＡ還元酵素阻害剤の中間体の製造方法
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
JP2010501643A (ja) 2007-07-12 2010-01-21 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 薄膜蒸発及び化学的手法によるロスバスタチン中間体の精製
EP2022784A1 (en) 2007-08-08 2009-02-11 LEK Pharmaceuticals D.D. Process for the preparation of methyl ester of rosuvastatin
EA201000214A1 (ru) 2007-08-28 2010-10-29 Рациофарм Гмбх Способ получения производных пентадикарбоновой кислоты
US8653265B2 (en) 2008-05-27 2014-02-18 Changzhou Pharmaceutical Factory Preparation method of rosuvastatin calcium and its intermediates
EP2350025A1 (en) * 2008-09-30 2011-08-03 Aurobindo Pharma Limited An improved process for preparing pyrimidine propenaldehyde
EP2752407B1 (en) 2009-01-14 2015-09-23 Krka Tovarna Zdravil, D.D., Novo Mesto Crystalline rosuvastatin calcium trihydrate
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
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
WO2013080219A2 (en) 2011-11-28 2013-06-06 Mylan Laboratories Ltd NOVEL PROCESS FOR THE PREPARATION OF INTERMEDIATES OF HMG-CoA REDUCTASE INHIBITORS
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)

* Cited by examiner, † Cited by third party
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
AU2002324715B2 (en) * 2001-08-16 2009-03-12 Teva Pharmaceutical Industries Ltd. Processes for preparing calcium salt forms of statins

Also Published As

Publication number Publication date
WO2003097614A3 (en) 2004-05-21
WO2003097614A2 (en) 2003-11-27
EP1585736A2 (en) 2005-10-19
US20050222415A1 (en) 2005-10-06
AU2003228010A1 (en) 2003-12-02
BR0311195A (pt) 2005-02-22
EA200401533A1 (ru) 2005-06-30

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