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EA200000511A1 - Способ получения циталопрама - Google Patents

Способ получения циталопрама

Info

Publication number
EA200000511A1
EA200000511A1 EA200000511A EA200000511A EA200000511A1 EA 200000511 A1 EA200000511 A1 EA 200000511A1 EA 200000511 A EA200000511 A EA 200000511A EA 200000511 A EA200000511 A EA 200000511A EA 200000511 A1 EA200000511 A1 EA 200000511A1
Authority
EA
Eurasian Patent Office
Prior art keywords
cytaloprama
obtaining
compound
formula
citalopram
Prior art date
Application number
EA200000511A
Other languages
English (en)
Other versions
EA002770B1 (ru
Inventor
Ханс Петерсен
Петер Брайнедаль
Клаус Петер Бегесе
Original Assignee
Х.Лундбекк А/С
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 Х.Лундбекк А/С filed Critical Х.Лундбекк А/С
Publication of EA200000511A1 publication Critical patent/EA200000511A1/ru
Publication of EA002770B1 publication Critical patent/EA002770B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C215/00—Compounds containing amino and hydroxy groups bound to the same carbon skeleton
    • C07C215/68—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having amino groups bound to carbon atoms of six-membered aromatic rings and hydroxy groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C225/00—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones
    • C07C225/22—Compounds containing amino groups and doubly—bound oxygen atoms bound to the same carbon skeleton, at least one of the doubly—bound oxygen atoms not being part of a —CHO group, e.g. amino ketones having amino groups bound to carbon atoms of six-membered aromatic rings of the carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/30—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms
    • C07C233/33—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by doubly-bound oxygen atoms with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C233/00—Carboxylic acid amides
    • C07C233/01—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms
    • C07C233/34—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups
    • C07C233/42—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring
    • C07C233/43—Carboxylic acid amides having carbon atoms of carboxamide groups bound to hydrogen atoms or to acyclic carbon atoms having the nitrogen atom of at least one of the carboxamide groups bound to a carbon atom of a hydrocarbon radical substituted by amino groups with the substituted hydrocarbon radical bound to the nitrogen atom of the carboxamide group by a carbon atom of a six-membered aromatic ring having the carbon atom of the carboxamide group bound to a hydrogen atom or to a carbon atom of a saturated carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D307/00—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom ortho- or peri-condensed with carbocyclic rings or ring systems
    • C07D307/87—Benzo [c] furans; Hydrogenated benzo [c] furans
    • C07D307/88—Benzo [c] furans; Hydrogenated benzo [c] furans with one oxygen atom directly attached in position 1 or 3

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Engineering & Computer Science (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Описан способ получения циталопрама, предусматривающий реакцию соединения формулы (IV), где Rпредставляет H или C-алкилкарбонил, последовательно с реактивом Гриньяра 4-галогенфторфенила и реактивом Гриньяра 3-галоген-N,N-диметилпропиламина, выполнение замыкания кольца полученного соединения формулы (VI) и превращение полученного 1,3-дигидроизобензофуранового соединения в соответствующее 5-цианопроизводное, т.е. циталопрам.Отчет о международном поиске был опубликован 1998.08.13.
EA200000511A 1997-11-11 1997-11-11 Способ получения циталопрама EA002770B1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CN97182416A CN1286687A (zh) 1997-11-11 1997-11-11 制备西酞普兰的方法
PCT/DK1997/000513 WO1998019512A2 (en) 1997-11-11 1997-11-11 Method for the preparation of citalopram

Publications (2)

Publication Number Publication Date
EA200000511A1 true EA200000511A1 (ru) 2000-10-30
EA002770B1 EA002770B1 (ru) 2002-08-29

Family

ID=37709785

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000511A EA002770B1 (ru) 1997-11-11 1997-11-11 Способ получения циталопрама

Country Status (20)

Country Link
US (1) US6258842B1 (ru)
EP (1) EP1042310B1 (ru)
JP (1) JP3813820B2 (ru)
CN (1) CN1286687A (ru)
AT (1) ATE221522T1 (ru)
AU (1) AU738359B2 (ru)
BR (1) BR9714925A (ru)
CA (1) CA2291072C (ru)
CZ (1) CZ292911B6 (ru)
DE (2) DE1042310T1 (ru)
DK (1) DK1042310T3 (ru)
EA (1) EA002770B1 (ru)
ES (1) ES2149734T3 (ru)
HU (1) HUP0002953A3 (ru)
IS (1) IS2009B (ru)
SK (1) SK283907B6 (ru)
TR (1) TR200001341T2 (ru)
UA (1) UA62984C2 (ru)
WO (1) WO1998019512A2 (ru)
ZA (1) ZA9810058B (ru)

Families Citing this family (57)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA62985C2 (en) 1997-11-10 2004-01-15 Lunnbeck As H A method for the preparation of citalopram
EA002977B1 (ru) * 1998-10-20 2002-12-26 Х.Лундбекк А/С Способ получения циталопрама
TR200101796T2 (tr) 1998-12-23 2001-11-21 H. Lundbeck A/S 5-Siyanofitalitin preparasyonuna yönelik metot
AR022329A1 (es) 1999-01-29 2002-09-04 Lundbeck & Co As H Metodo para la preparacion de 5-cianoftalida
NZ514671A (en) 1999-04-14 2003-10-31 H Method for the preparation of citalopram
US6245782B1 (en) 1999-05-17 2001-06-12 Heartdrug Research L.L.C. Methods of inhibiting platelet activation with selective serotonin reuptake inhibitors
ITMI991579A1 (it) 1999-06-25 2001-01-15 Lundbeck & Co As H Metodo per la preparazione di citalopram
ITMI991581A1 (it) * 1999-06-25 2001-01-15 Lundbeck & Co As H Metodo per la preparazione di citalopram
ITMI991486A1 (it) * 1999-07-06 2001-01-06 Vis Farmaceutici S P A Processo per la sintesi di citalopram
AR021155A1 (es) * 1999-07-08 2002-06-12 Lundbeck & Co As H Tratamiento de desordenes neuroticos
AU742554B2 (en) 1999-10-25 2002-01-03 H. Lundbeck A/S Method for the preparation of citalopram
DK1228056T3 (da) 1999-10-25 2005-01-24 Lundbeck & Co As H Fremgangsmåde til fremstilling af citalopram
AR026063A1 (es) 1999-11-01 2002-12-26 Lundbeck & Co As H Metodo para la preparacion de 5-carboxiftalida.
DE69915713T2 (de) 1999-12-28 2005-03-03 H. Lundbeck A/S Verfahren zur herstellung von citalopram
HK1052512B (zh) * 1999-12-30 2006-03-03 H. 隆德贝克有限公司 西酞普兰的制备方法
SK286879B6 (sk) 2000-01-14 2009-07-06 H. Lundbeck A/S Spôsob prípravy 5-kyanoftalidu
FR2805812A1 (fr) 2000-02-24 2001-09-07 Lundbeck & Co As H Procede de preparation du citalopram
IES20010157A2 (en) 2000-03-03 2002-03-06 Lundbeck & Co As H Method for the preparation of citalopram
GB0005477D0 (en) 2000-03-07 2000-04-26 Resolution Chemicals Limited Process for the preparation of citalopram
AU2001242298A1 (en) 2000-03-13 2001-09-24 H Lunbeck A/S Method for the preparation of citalopram
WO2001068629A1 (en) 2000-03-13 2001-09-20 H. Lundbeck A/S Stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans
NL1017500C1 (nl) 2000-03-13 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van Citalopram.
GB2357762B (en) * 2000-03-13 2002-01-30 Lundbeck & Co As H Crystalline base of citalopram
DE60101786T2 (de) 2000-03-14 2004-07-15 H. Lundbeck A/S, Valby Verfahren zur herstellung von citalopram
DE10190485T1 (de) * 2000-03-16 2002-03-21 Lundbeck & Co As H Verfahren zur Herstellung von 5-Cyano-1-(4-fluorphenyl)-1,3-dihydroisobenzofuranen
AR032455A1 (es) * 2000-05-12 2003-11-12 Lundbeck & Co As H Metodo para la preparacion de citalopram, un intermediario empleado en el metodo, un metodo para la preparacion del intermediario empleado en el metodo y composicion farmaceutica antidepresiva
US6879110B2 (en) * 2000-07-27 2005-04-12 Semiconductor Energy Laboratory Co., Ltd. Method of driving display device
IL144817A0 (en) * 2000-08-18 2002-06-30 Lundbeck & Co As H Method for the preparation of citalopram
IT1319686B1 (it) * 2000-12-12 2003-10-23 C D Farmasint S R L Procedimento di preparazione di citalopram.
CN1282648C (zh) 2000-12-22 2006-11-01 H·隆德贝克有限公司 制备纯西酞普兰的方法
DE10112828C1 (de) * 2000-12-28 2002-11-21 Lundbeck & Co As H Verfahren zur Herstellung von Citalopram
KR100430746B1 (ko) * 2000-12-28 2004-05-10 하. 룬트벡 아크티에 셀스카브 순수한 시탈로프람의 제조방법
EP1355897A1 (en) 2001-01-30 2003-10-29 Orion Corporation Fermion Process for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile
CZ20033267A3 (en) * 2001-05-01 2004-06-16 H. Lundbeck A/S The use of enantiomeric pure escitalopram
BG65271B1 (bg) * 2001-06-18 2007-11-30 H. Lundbeck A/S Метод за получаване на циталопрам
EP1522539B1 (en) * 2001-07-31 2007-01-24 H. Lundbeck A/S Crystalline composition containing escitalopram
IS7239A (is) * 2001-12-14 2004-04-29 H. Lundbeck A/S Aðferð til framleiðslu á essítalóprami
AU2003222435A1 (en) 2002-01-07 2003-07-24 Sun Pharmaceutical Industries Limited Process for the preparation of 1-(3-(dimethylamino)propyl)-1-(4-fluorophenyl)- 1,3-dihydro-5-isobenzofuran carbonitrile
HU0200980D0 (ru) 2002-03-14 2002-05-29 Gabor S Pal Dr
BG65515B1 (bg) * 2002-07-26 2008-10-31 H. Lundbeck A/S Метод за получаване на 5-цианофталид
TWI306846B (en) 2002-08-12 2009-03-01 Lundbeck & Co As H Method for the separation of intermediates which may be used for the preparation of escitalopram
US6812355B2 (en) 2002-10-22 2004-11-02 Sekhsaria Chemicals Limited Process for the manufacture of citalopram hydrobromide from 5-bromophthalide
ITMI20030479A1 (it) * 2003-03-13 2004-09-14 Adorkem Technology S P A Procedimento per la preparazione di un ciano-isobenzofurano.
US6781003B1 (en) * 2003-06-09 2004-08-24 Aurobindo Pharma Ltd. Preparation of pure citalopram
EP1486492A3 (en) 2003-06-10 2005-02-23 Sun Pharmaceuticals Industries Ltd. A process for hydrogenolysis of [1-(3-dimethylamino)propyl)]-1-(4-fluorophenyl)-1,3-dihydro-5-halo-isobenzofuran.
SI1506963T1 (en) * 2003-10-28 2005-10-31 Adorkem Technology Spa Method for the preparation of citalopram
CN100569765C (zh) 2003-12-19 2009-12-16 杭州民生药业集团有限公司 西酞普兰中间体晶体碱
KR101166280B1 (ko) 2004-08-23 2013-11-27 썬 파마 글로벌 에프제트이 시탈로프램 및 에난티오머의 제조 방법
WO2006103550A1 (en) * 2005-03-31 2006-10-05 Ranbaxy Laboratories Limited Processes for the preparation of citalopram and its intermediate 5-aminophthalide
TWI358407B (en) 2005-06-22 2012-02-21 Lundbeck & Co As H Crystalline base of escitalopram and orodispersibl
US7834201B2 (en) 2005-06-22 2010-11-16 H. Lundbeck A/S Crystalline base of escitalopram and orodispersible tablets comprising escitalopram base
CN100391952C (zh) * 2005-07-12 2008-06-04 广东西陇化工有限公司 西酞普兰盐的制备方法
WO2009111031A2 (en) * 2008-03-04 2009-09-11 Intra-Cellular Therapies, Inc. Methods of treating vasomotor symptoms
CN105801328B (zh) * 2016-04-29 2017-12-08 浙江瑞灿科技有限公司 一种晕苯的制备方法
CN105801333B (zh) * 2016-04-29 2017-12-22 江苏佳麦化工有限公司 一种晕苯的制备方法
CN105801329B (zh) * 2016-04-29 2017-11-28 阜阳欣奕华材料科技有限公司 一种晕苯的制备方法
CN106748627A (zh) * 2016-11-14 2017-05-31 苏州市罗森助剂有限公司 一种一锅法制备3,5‑二甲基溴苯的方法

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Publication number Priority date Publication date Assignee Title
GB1143702A (ru) 1965-03-18
GB1526331A (en) * 1976-01-14 1978-09-27 Kefalas As Phthalanes
GB8419963D0 (en) * 1984-08-06 1984-09-12 Lundbeck & Co As H Intermediate compound and method
NZ243065A (en) 1991-06-13 1995-07-26 Lundbeck & Co As H Piperidine derivatives and pharmaceutical compositions
UA62985C2 (en) 1997-11-10 2004-01-15 Lunnbeck As H A method for the preparation of citalopram

Also Published As

Publication number Publication date
BR9714925A (pt) 2003-07-22
AU5116898A (en) 1998-05-29
CN1286687A (zh) 2001-03-07
UA62984C2 (en) 2004-01-15
EP1042310B1 (en) 2002-07-31
WO1998019512A3 (en) 1998-08-13
ZA9810058B (en) 1999-05-05
AU738359B2 (en) 2001-09-13
DK1042310T3 (da) 2002-12-02
ES2149734T3 (es) 2003-02-16
WO1998019512A2 (en) 1998-05-14
EA002770B1 (ru) 2002-08-29
IS2009B (is) 2005-05-13
TR200001341T2 (tr) 2000-11-21
ES2149734T1 (es) 2000-11-16
DE69714480D1 (de) 2002-09-05
HUP0002953A3 (en) 2002-12-28
CA2291072C (en) 2002-08-20
JP2002530295A (ja) 2002-09-17
US6258842B1 (en) 2001-07-10
CZ292911B6 (cs) 2004-01-14
SK6822000A3 (en) 2000-10-09
DE1042310T1 (de) 2001-04-19
JP3813820B2 (ja) 2006-08-23
IS5461A (is) 2000-04-18
CA2291072A1 (en) 1998-05-14
HUP0002953A2 (hu) 2001-04-28
CZ20001736A3 (cs) 2000-10-11
ATE221522T1 (de) 2002-08-15
DE69714480T2 (de) 2003-03-06
SK283907B6 (sk) 2004-04-06
EP1042310A2 (en) 2000-10-11

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MM4A Lapse of a eurasian patent due to non-payment of renewal fees within the time limit in the following designated state(s)

Designated state(s): AM AZ KZ KG MD TJ TM