AR048271A1 - Procesos para la produccion de calcio de atorvastatina en forma amorfa - Google Patents
Procesos para la produccion de calcio de atorvastatina en forma amorfaInfo
- Publication number
- AR048271A1 AR048271A1 ARP050101018A ARP050101018A AR048271A1 AR 048271 A1 AR048271 A1 AR 048271A1 AR P050101018 A ARP050101018 A AR P050101018A AR P050101018 A ARP050101018 A AR P050101018A AR 048271 A1 AR048271 A1 AR 048271A1
- Authority
- AR
- Argentina
- Prior art keywords
- atorvastatin calcium
- calcium
- atorvastatin
- amorphous form
- alkali metal
- Prior art date
Links
Classifications
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
- C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D207/30—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two double bonds between ring members or between ring members and non-ring members
- C07D207/34—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having two 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, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P3/00—Drugs for disorders of the metabolism
- A61P3/06—Antihyperlipidemics
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Obesity (AREA)
- Diabetes (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Hematology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pyrrole Compounds (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Abstract
Reivindicacion 1: Un proceso para la produccion de calcio de atorvastatina en forma amorfa que comprende: a) reaccionar una solucion de (4R-cis)-1,1-dimetiletil-6-{2-[2-(4-fluorofenil)-5-(1-metiletil)-3-fenil-4-[(fenilamino)-carbonil]-1H-pirrol- 1il]etil}-2,2-dimetil-1,3-dioxano-4-acetato (Compuesto H) en un solvente miscible en agua con un ácido para obtener [R-(R*,R*)]-1,1-dimetiletil-2-(4-fluorofenil)-beta, delta-dihidroxi-5-(1-metiletil)-3-fenil-4-[(fenilamino) carbonil]-1H-pirrole-1- heptanoato (Compuesto I); b) tratar el Compuesto I con un hidroxido metálico álcali para obtener una sal metálica álcali de atorvastatina; c) lavar la solucion de sal metálica álcali de astorvastatina con un solvente no miscible o levemente miscible en agua; d) tratar la solucion lavada de sal metálica álcali de atorvastatina con una sal de calcio o hidroxido de calcio para obtener calcio de atorvastatina; e) aislar el calcio de atorvastatina crudo; f) purificar el calcio de atorvastatina crudo mediante la disolucion en una mezcla de tetrahidrofurano y metanol, y precipitando con agua para obtener calcio de atorvastatina puro en forma cristalina; y g) convertir el calcio de atorvastatina cristalino puro así obtenido en forma amorfa. Reivindicacion 29: UN proceso para la produccion de calcio de atorvastatina estabilizado, en forma amorfa que comprende: a) La disolucion del calcio de atorvastatina cristalino y un antioxidante en un solvente; b) El agregado de calcio de atorvastatina y solucion antioxidante a un antisolvente y c) La separacion del calcio de atorvastatina precipitado, en forma amorfa de la suspension resultante para obtener calcio de atorvastatina estabilizado, en forma amorfa.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
IN491DE2004 | 2004-03-17 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR048271A1 true AR048271A1 (es) | 2006-04-12 |
Family
ID=33516010
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP050101018A AR048271A1 (es) | 2004-03-17 | 2005-03-16 | Procesos para la produccion de calcio de atorvastatina en forma amorfa |
Country Status (17)
Country | Link |
---|---|
US (1) | US7994343B2 (es) |
EP (3) | EP1577297A1 (es) |
CN (2) | CN1942439B (es) |
AR (1) | AR048271A1 (es) |
AT (1) | ATE545629T1 (es) |
AU (2) | AU2004317570B2 (es) |
CA (3) | CA2560252C (es) |
CY (1) | CY1112583T1 (es) |
DK (1) | DK1727795T3 (es) |
ES (1) | ES2381473T3 (es) |
FI (1) | FI120344B (es) |
MY (1) | MY147435A (es) |
NO (1) | NO330092B1 (es) |
PL (1) | PL1727795T3 (es) |
PT (1) | PT1727795E (es) |
SI (1) | SI1727795T1 (es) |
WO (1) | WO2005092852A1 (es) |
Families Citing this family (34)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
EP1577297A1 (en) * | 2004-03-17 | 2005-09-21 | Ranbaxy Laboratories, Ltd. | Process for the production of atorvastatin calcium in amorphous form |
JP5000502B2 (ja) * | 2004-07-16 | 2012-08-15 | レツク・フアーマシユーテイカルズ・デー・デー | アトルバスタチンカルシウムの酸化分解生成物 |
JP2008510798A (ja) * | 2004-08-27 | 2008-04-10 | バイオコン・リミテッド | 非晶質アトルバスタチンカルシウムのための方法 |
GB2424880A (en) * | 2005-04-06 | 2006-10-11 | Generics | Crystalline forms of atorvastatin sodium, processes for their preparation and their use in inhibiting HMG-CoA reductase |
WO2007020413A1 (en) | 2005-08-15 | 2007-02-22 | Arrow International Limited | Crystalline and amorphous sodium atorvastatin |
WO2007020421A1 (en) | 2005-08-15 | 2007-02-22 | Arrow International Limited | Crystalline and amorphous sodium atorvastatin |
GB0613567D0 (en) * | 2006-07-07 | 2006-08-16 | Arrow Int Ltd | Crystalline sodium atorvastatin |
GB0613566D0 (en) * | 2006-07-07 | 2006-08-16 | Arrow Int Ltd | Crystalline sodium atorvastatin |
ES2270722B1 (es) * | 2005-09-15 | 2008-03-01 | Ercros Industrial, S.A. | Procedimiento para la obtencion de atorvastatina calcica amorfa. |
GB0523637D0 (en) * | 2005-11-21 | 2005-12-28 | Avecia Pharmaceuticals Ltd | Process and compounds |
WO2007099552A2 (en) * | 2006-03-02 | 2007-09-07 | Matrix Labaratories Ltd | Novel crystalline form of atovastatin hemi-magnesium |
SI22255A (sl) * | 2006-04-14 | 2007-10-31 | Krka, Tovarna Zdravil, D.D., Novo Mesto | Novi polimorfi statinovih soli in njihova uporabav farmacevtskih formulacijah |
CN101205209B (zh) * | 2007-12-25 | 2010-06-02 | 浙江新东港药业股份有限公司 | 一种阿伐他汀中间体的精制方法 |
EP2075246A1 (en) * | 2007-12-27 | 2009-07-01 | M. J. Institute of Research | A process for preparation of amorphous form of atorvastatin hemi-calcium salt |
CN101468963B (zh) * | 2007-12-28 | 2012-09-19 | 石药集团中奇制药技术(石家庄)有限公司 | 一种无定形阿伐他汀钙的制备方法 |
KR100850558B1 (ko) * | 2008-01-02 | 2008-08-06 | 조동옥 | 아토르바스타틴의 효율적인 제조방법 |
CN101560177B (zh) * | 2008-04-16 | 2012-10-03 | 北京万全阳光医学技术有限公司 | 一种阿托伐他汀钙的制备方法 |
CN101429195B (zh) * | 2008-11-03 | 2010-12-15 | 华东师范大学 | 一种高纯度阿托伐他汀重要合成中间体的制备方法 |
US8115015B2 (en) | 2009-01-26 | 2012-02-14 | Cadila Healthcare Limited | Process for the preparation of amorphous atorvastatin calcium |
WO2011131605A1 (en) * | 2010-04-19 | 2011-10-27 | Dsm Ip Assets B.V. | Production of atorvastatin low in ether impurities |
CN102127060B (zh) * | 2010-12-17 | 2013-12-04 | 蚌埠丰原医药科技发展有限公司 | 一种阿托伐他汀钙中间体的制备方法 |
CN102070504A (zh) * | 2010-12-23 | 2011-05-25 | 蚌埠丰原医药科技发展有限公司 | 阿托伐他汀钠的制备方法 |
CN102070505B (zh) * | 2011-01-28 | 2012-01-11 | 海南美大制药有限公司 | 阿托伐他汀钙化合物及其新制法 |
CN103483238B (zh) * | 2013-08-20 | 2014-12-31 | 蚌埠丰原医药科技发展有限公司 | 阿托伐他汀钙三水合物的制备方法 |
CN104945300B (zh) * | 2015-06-17 | 2017-05-10 | 北京嘉林药业股份有限公司 | 一种ⅰ型阿托伐他汀钙的纯化方法 |
WO2017060885A1 (en) * | 2015-10-09 | 2017-04-13 | Laurus Labs Private Limited | An improved process for preparation of atorvastatin or pharmaceutically acceptable salts thereof |
CN106478591B (zh) * | 2016-09-30 | 2018-11-13 | 北京嘉林药业股份有限公司 | 一种阿托伐他汀缩合物中间体的拆分方法 |
CN106432033B (zh) * | 2016-10-21 | 2018-07-27 | 江苏阿尔法药业有限公司 | 一种无定形阿托伐他汀钙的制备方法 |
CN108033899B (zh) * | 2017-12-06 | 2020-04-10 | 浙江科技学院 | 一种(r)-6-氰基-5-羟基-3-羰基己酸叔丁酯的制备方法 |
CN109232355A (zh) * | 2018-10-09 | 2019-01-18 | 河南师范大学 | 一种有效去除阿托伐他汀钙粗品中杂质阿托伐他汀缩合物的方法 |
CN109280024A (zh) * | 2018-10-09 | 2019-01-29 | 河南师范大学 | 一种高纯度阿托伐他汀叔丁酯的制备方法 |
CN110563628B (zh) * | 2019-08-26 | 2022-04-05 | 北京嘉林药业股份有限公司 | 一种双釜制备高纯度和单分散i晶型阿托伐他汀钙的结晶方法 |
CN110776451B (zh) * | 2020-01-02 | 2020-05-22 | 湖南迪诺制药股份有限公司 | 一种i晶型阿托伐他汀钙的制备方法 |
CN113695307B (zh) * | 2020-05-20 | 2022-12-02 | 天津嘉林科医有限公司 | 一种盛放阿托伐他汀钙的玻璃器皿的清洗方法 |
Family Cites Families (36)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
US5245047A (en) | 1988-02-22 | 1993-09-14 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
US5216174A (en) | 1988-02-22 | 1993-06-01 | Warner-Lambert Co. | Process for trans-6-[12-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
US5124482A (en) | 1988-02-22 | 1992-06-23 | Warner-Lambert Company | Process for trans-6-(2-substituted-pyrrol-1-yl)alkyl)pyran-2-one inhibitors of cholesterol synthesis |
US5149837A (en) | 1988-02-22 | 1992-09-22 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
US5003080A (en) | 1988-02-22 | 1991-03-26 | Warner-Lambert Company | Process for trans-6-(2-(substituted-pyrrol-1-yl)alkyl)pryan-2-one inhibitors of cholesterol synthesis |
US5097045A (en) | 1989-02-01 | 1992-03-17 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
FI94339C (fi) | 1989-07-21 | 1995-08-25 | Warner Lambert Co | Menetelmä farmaseuttisesti käyttökelpoisen /R-(R*,R*)/-2-(4-fluorifenyyli)- , -dihydroksi-5-(1-metyylietyyli)-3-fenyyli-4-/(fenyyliamino)karbonyyli/-1H-pyrroli-1-heptaanihapon ja sen farmaseuttisesti hyväksyttävien suolojen valmistamiseksi |
US5103024A (en) | 1990-10-17 | 1992-04-07 | Warner-Lambert Company | Process for the synthesis of (4r-cis)-1,1-dimethylethyl 6-cyanomethyl-2,2-dimethyl-1,3-dioxane-4-acetate |
US5248793A (en) | 1990-10-17 | 1993-09-28 | Warner-Lambert Company | Process for the synthesis of (4R-cis)-1,1-dimethylethyl 6-iodomethyl or 6-(phenyl-substituted)sulfonyloxymethyl-2,2-dimethyl-1,3-dioxane-4-acetate |
US5155251A (en) | 1991-10-11 | 1992-10-13 | Warner-Lambert Company | Process for the synthesis of (5R)-1,1-dimethylethyl-6-cyano-5-hydroxy-3-oxo-hexanoate |
WO1994016693A1 (en) * | 1993-01-19 | 1994-08-04 | Warner-Lambert Company | Stable oral ci-981 formulation and process of preparing same |
US5298627A (en) | 1993-03-03 | 1994-03-29 | Warner-Lambert Company | Process for trans-6-[2-(substituted-pyrrol-1-yl)alkyl]pyran-2-one inhibitors of cholesterol synthesis |
IL128862A (en) | 1995-07-17 | 2007-12-03 | Warner Lambert Co | [R - (R * R *)] - 2 - (4 - fluorophenyl) - ß, d - dihydroxy - 5 - (1 - methyl - ethyl) 3 - phenyl - 4 - [(phenamino) carbonyl)] - 1H - Pyrol - 1 - Patenoic acid Hydrogen salt Hydrogen crystalline (Atorostatin) Crystalline hydrate |
HRP960312B1 (en) * | 1995-07-17 | 2001-10-31 | Warner Lambert Co | NOVEL PROCESS FOR THE PRODUCTION OF AMORPHOUS /R-(R*, R*)/-2-(4-FLUOROPHENYL)-"beta", "delta"-DIHYDROXY-5-PHENYL-4-/(PHENYLAMINO)CARBONYL/-1H-PYRROLE -1-HEPTANOIC ACID CALCIUM SALT (2 : 1) |
IN191236B (es) | 1999-05-25 | 2003-10-11 | Ranbaxy Lab Ltd | |
US6646133B1 (en) * | 2000-10-17 | 2003-11-11 | Egis Gyogyszergyar Rt. | Process for the preparation of amorphous atorvastatin calcium |
HU226640B1 (en) | 1999-10-18 | 2009-05-28 | Egis Gyogyszergyar Nyilvanosan | Process for producing amorphous atorvastatin calcium salt |
SI20425A (sl) * | 1999-12-10 | 2001-06-30 | LEK tovarna farmacevtskih in kemi�nih izdelkov d.d. | Priprava amorfnega atorvastatina |
JP2004501121A (ja) | 2000-06-09 | 2004-01-15 | エルイーケー ファーマシューティカルズ ディー.ディー. | 安定した医薬効果を有する合成物、及びそれを含む医薬製剤 |
IL155734A0 (en) | 2000-11-03 | 2003-11-23 | Teve Pharmaceutical Ind Ltd | Atorvastatin hemi-calcium form vii |
IL156055A0 (en) | 2000-11-30 | 2003-12-23 | Teva Pharma | Novel crystal forms of atorvastatin hemi calcium and processes for their preparation as well as novel processes for preparing other forms |
AU2002246675A1 (en) | 2000-12-18 | 2002-07-30 | Merck And Co., Inc. | Thrombin inhibitors |
CZ20032019A3 (cs) | 2000-12-27 | 2003-10-15 | Ciba Specialty Chemicals Holding Inc. | Krystalické formy Atorvastatinu |
WO2002057228A1 (en) | 2001-01-17 | 2002-07-25 | Biocon India Limited | Atorvastatin calcium |
SI20814A (sl) | 2001-01-23 | 2002-08-31 | LEK, tovarna farmacevtskih in kemi�nih izdelkov, d.d. | Priprava amorfnega atorvastatina |
IN190564B (es) * | 2001-04-11 | 2003-08-09 | Cadila Heathcare Ltd | |
EA005317B1 (ru) | 2001-06-29 | 2004-12-30 | УОРНЕР-ЛАМБЕРТ КОМПАНИ Эл-Эл-Си | Кристаллические формы [r-(r*,r*)]-2-(4-фторфенил)-бета, дельта-дигидрокси-5-(1-метилэтил)-3-фенил-4-[(фениламино)карбонил]-1h-пиррол-1-гептановой кислоты кальциевой соли (2:1) (аторвастатин) |
EP1414796A1 (en) | 2001-07-30 | 2004-05-06 | Dr. Reddy's Laboratories Ltd. | Crystalline forms vi and vii of atorvastatin calcium |
US7563911B2 (en) | 2001-08-31 | 2009-07-21 | Morepen Laboratories Ltd. | Process for the preparation of amorphous atorvastin calcium salt (2:1) |
CZ296967B6 (cs) * | 2002-02-01 | 2006-08-16 | Zentiva, A.S. | Zpusob výroby amorfní formy hemivápenaté soli (3R,5R) 7-[3-fenyl-4-fenylkarbamoyl-2-(4-fluorfenyl)-5-isopropylpyrrol-1-yl]-3,5-dihydroxyheptanové kyseliny (atorvastatinu) |
ATE452871T1 (de) | 2002-03-18 | 2010-01-15 | Biocon Ltd | Amorphe hmg-coa-reduktase-inhibitoren mit gewünschter teilchengrösse |
WO2003099785A1 (en) | 2002-05-28 | 2003-12-04 | Cadila Healthcare Limited | Process for the preparation of amorphous atorvastatin calcium |
SI21302A (sl) | 2002-10-11 | 2004-04-30 | LEK farmacevtska dru�ba d.d. | Stabiliziran farmacevtski izdelek z amorfno aktivno učinkovino |
HU227041B1 (en) | 2003-03-24 | 2010-05-28 | Richter Gedeon Nyrt | Process for the synthesis of amorphous atorvastatin calcium |
EP1577297A1 (en) * | 2004-03-17 | 2005-09-21 | Ranbaxy Laboratories, Ltd. | Process for the production of atorvastatin calcium in amorphous form |
CN101124230A (zh) | 2004-09-28 | 2008-02-13 | 特瓦制药工业有限公司 | 制备基本无杂质的阿托伐他汀钙形式的方法 |
-
2004
- 2004-11-19 EP EP04027584A patent/EP1577297A1/en not_active Withdrawn
- 2004-11-19 NO NO20045037A patent/NO330092B1/no not_active IP Right Cessation
- 2004-11-19 CA CA002560252A patent/CA2560252C/en not_active Expired - Fee Related
- 2004-11-19 CA CA002666359A patent/CA2666359A1/en not_active Abandoned
- 2004-11-19 AT AT04798913T patent/ATE545629T1/de active
- 2004-11-19 ES ES04798913T patent/ES2381473T3/es active Active
- 2004-11-19 DK DK04798913.2T patent/DK1727795T3/da active
- 2004-11-19 CA CA002627940A patent/CA2627940A1/en not_active Abandoned
- 2004-11-19 FI FI20041489A patent/FI120344B/fi not_active IP Right Cessation
- 2004-11-19 AU AU2004317570A patent/AU2004317570B2/en not_active Ceased
- 2004-11-19 SI SI200431843T patent/SI1727795T1/sl unknown
- 2004-11-19 EP EP04798913A patent/EP1727795B1/en active Active
- 2004-11-19 US US10/549,890 patent/US7994343B2/en not_active Expired - Fee Related
- 2004-11-19 CN CN2004800428343A patent/CN1942439B/zh not_active Expired - Fee Related
- 2004-11-19 PT PT04798913T patent/PT1727795E/pt unknown
- 2004-11-19 PL PL04798913T patent/PL1727795T3/pl unknown
- 2004-11-19 WO PCT/IB2004/003789 patent/WO2005092852A1/en active Application Filing
-
2005
- 2005-03-16 AR ARP050101018A patent/AR048271A1/es unknown
- 2005-03-17 CN CNA200580012704XA patent/CN1946688A/zh active Pending
- 2005-03-17 MY MYPI20051161A patent/MY147435A/en unknown
- 2005-09-16 EP EP05077109A patent/EP1659110A1/en not_active Ceased
-
2010
- 2010-12-03 AU AU2010249166A patent/AU2010249166B2/en not_active Ceased
-
2012
- 2012-04-04 CY CY20121100335T patent/CY1112583T1/el unknown
Also Published As
Publication number | Publication date |
---|---|
PT1727795E (pt) | 2012-04-11 |
CN1946688A (zh) | 2007-04-11 |
EP1577297A1 (en) | 2005-09-21 |
FI20041489A (fi) | 2006-07-20 |
CN1942439B (zh) | 2011-12-21 |
CA2560252C (en) | 2009-08-04 |
CA2560252A1 (en) | 2005-10-06 |
EP1659110A1 (en) | 2006-05-24 |
US20100197941A1 (en) | 2010-08-05 |
WO2005092852A1 (en) | 2005-10-06 |
US7994343B2 (en) | 2011-08-09 |
AU2010249166B2 (en) | 2012-02-09 |
FI20041489A0 (fi) | 2004-11-19 |
ATE545629T1 (de) | 2012-03-15 |
CN1942439A (zh) | 2007-04-04 |
NO20045037L (no) | 2005-09-19 |
SI1727795T1 (sl) | 2012-05-31 |
MY147435A (en) | 2012-12-14 |
EP1727795B1 (en) | 2012-02-15 |
AU2004317570A1 (en) | 2005-10-06 |
EP1727795A1 (en) | 2006-12-06 |
FI120344B (fi) | 2009-09-30 |
ES2381473T3 (es) | 2012-05-28 |
AU2010249166A1 (en) | 2010-12-23 |
NO20045037D0 (no) | 2004-11-19 |
AU2004317570B2 (en) | 2011-01-06 |
CY1112583T1 (el) | 2016-02-10 |
CA2627940A1 (en) | 2005-10-06 |
NO330092B1 (no) | 2011-02-14 |
DK1727795T3 (da) | 2012-04-16 |
CA2666359A1 (en) | 2005-10-06 |
PL1727795T3 (pl) | 2012-06-29 |
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