EA200100457A1 - Способ получения циталопрама - Google Patents

Способ получения циталопрама

Info

Publication number
EA200100457A1
EA200100457A1 EA200100457A EA200100457A EA200100457A1 EA 200100457 A1 EA200100457 A1 EA 200100457A1 EA 200100457 A EA200100457 A EA 200100457A EA 200100457 A EA200100457 A EA 200100457A EA 200100457 A1 EA200100457 A1 EA 200100457A1
Authority
EA
Eurasian Patent Office
Prior art keywords
citalopram
alkyl
hydrogen
ring
spiro
Prior art date
Application number
EA200100457A
Other languages
English (en)
Other versions
EA002977B1 (ru
Inventor
Леоне Далль Аста
Умберто Казацца
Ханс Петерсен
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
Priority claimed from IT002242 external-priority patent/IT1302700B1/it
Priority claimed from IT1999MI001152 external-priority patent/IT1312319B1/it
Priority claimed from IT99MI001724 external-priority patent/IT1313587B1/it
Application filed by Х.Лундбекк А/С filed Critical Х.Лундбекк А/С
Publication of EA200100457A1 publication Critical patent/EA200100457A1/ru
Publication of EA002977B1 publication Critical patent/EA002977B1/ru

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D263/00—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D263/10—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
    • C07D263/14—Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms with radicals substituted by oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond

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)
  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

Настоящее изобретение относится к способу получения циталопрама или любого из его энантиомеров или кислотно-аддитивных солей, предусматривающему обработку соединения формулыв которой X представляет O или S; каждый из R1-R2 независимо выбран из водорода и Cалкила, или R1 и R2 вместе образуют Cалкиленовую цепь с образованием спиро-кольца; R выбран из водорода и Cалкила, R4 выбран из водорода, Cалкила, карбоксигруппы или группы-предшественника, либо R3 и R4 вместе образуют Cалкиленовую цепь с образованием спиро-кольца; дегидратирующим агентом; или альтернативно, когда X представляет S, термическое разложение тиазолинового кольца или обработку в присутствии инициатора свободных радикалов с образованием циталопрама. Изобретение также относится к промежуточным соединениям, используемым в новом способе получения циталопрама, а также к циталопраму, полученному с помощью нового способа.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200100457A 1998-10-20 1999-10-19 Способ получения циталопрама EA002977B1 (ru)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
IT002242 IT1302700B1 (it) 1998-10-20 1998-10-20 Procedimento per la preparazione di un derivato dell'isobenzofurano
IT1999MI001152 IT1312319B1 (it) 1999-05-25 1999-05-25 Procedimento per la preparazione del citalopram.
IT99MI001724 IT1313587B1 (it) 1999-08-02 1999-08-02 Procedimento per la preparazione di un derivato del5-cianoisobenzofurano.
PCT/DK1999/000576 WO2000023431A1 (en) 1998-10-20 1999-10-19 Method for the preparation of citalopram

Publications (2)

Publication Number Publication Date
EA200100457A1 true EA200100457A1 (ru) 2001-10-22
EA002977B1 EA002977B1 (ru) 2002-12-26

Family

ID=27274104

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200100457A EA002977B1 (ru) 1998-10-20 1999-10-19 Способ получения циталопрама

Country Status (25)

Country Link
US (1) US6365747B1 (ru)
EP (1) EP1123284B1 (ru)
JP (1) JP3892667B2 (ru)
KR (1) KR100411505B1 (ru)
CN (1) CN1129592C (ru)
AR (1) AR018693A1 (ru)
AT (1) ATE230738T1 (ru)
AU (1) AU746665B2 (ru)
BG (1) BG64704B1 (ru)
BR (1) BR9915158B1 (ru)
CA (1) CA2291134C (ru)
CZ (1) CZ299920B6 (ru)
DE (1) DE69904853T2 (ru)
DK (1) DK1123284T3 (ru)
EA (1) EA002977B1 (ru)
ES (1) ES2189502T3 (ru)
HK (1) HK1042297B (ru)
HU (1) HU228576B1 (ru)
IL (1) IL142346A0 (ru)
IS (1) IS2256B (ru)
NO (1) NO327038B1 (ru)
NZ (1) NZ510858A (ru)
PL (1) PL199423B1 (ru)
SK (1) SK285719B6 (ru)
WO (1) WO2000023431A1 (ru)

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2356188C (en) 1998-12-23 2006-05-23 H. Lundbeck A/S Method for the preparation of 5-cyanophthalide
AR022329A1 (es) 1999-01-29 2002-09-04 Lundbeck & Co As H Metodo para la preparacion de 5-cianoftalida
TR200102957T2 (tr) 1999-04-14 2004-12-21 H. Lundbeck A/S Sitalopram hazırlanması için metod.
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
AR021155A1 (es) * 1999-07-08 2002-06-12 Lundbeck & Co As H Tratamiento de desordenes neuroticos
ES2169709A1 (es) 1999-10-25 2002-07-01 Lundbeck & Co As H Metodo para la preparacion de citalopram
DK1298124T3 (da) 1999-10-25 2007-07-09 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.
SI1246812T1 (en) 1999-12-28 2004-08-31 H. Lundbeck A/S Method for the preparation of citalopram
PT1246813E (pt) 1999-12-30 2004-02-27 Lundbeck & Co As H Metodo para a preparacao de citalopram
EA005134B1 (ru) * 2000-01-14 2004-12-30 Х.Лундбекк А/С Способ получения 5-цианофталида
IT1317729B1 (it) * 2000-01-18 2003-07-15 Norpharma S P A Procedimento per la preparazione della 5-carbossiftalide.
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
IES20010206A2 (en) 2000-03-13 2002-03-06 Lundbeck & Co As H Method for the preparation of citalopram
NZ521201A (en) * 2000-03-13 2004-02-27 H Method for the preparation of citalopram
CN1427835A (zh) * 2000-03-13 2003-07-02 H·隆德贝克有限公司 5－取代的1－(4－氟苯基)－1,3－二氢异苯并呋喃的分步烷基化
GB2357762B (en) * 2000-03-13 2002-01-30 Lundbeck & Co As H Crystalline base of citalopram
ATE257832T1 (de) 2000-03-14 2004-01-15 Lundbeck & Co As H Verfahren zur herstellung von citalopram
WO2001068632A1 (en) * 2000-03-16 2001-09-20 H. Lundbeck A/S Method for the preparation of 5-cyano-1-(4-fluorophenyl)-1,3-dihydroisobenzofurans
US6977306B2 (en) 2000-05-02 2005-12-20 Sumitomo Chemical Company, Limited Citalopram hydrobromide crystal and method for crystallization thereof
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
IL144817A0 (en) 2000-08-18 2002-06-30 Lundbeck & Co As H Method for the preparation of citalopram
EP1181713B1 (en) 2000-12-22 2004-09-29 H. Lundbeck A/S Method for the preparation of pure citalopram
PT1181272E (pt) 2000-12-28 2003-01-31 Lundbeck & Co As H Processo para a preparacao de citalopram puro
WO2002060886A1 (en) 2001-01-30 2002-08-08 Orion Corporation, Fermion Process for the preparation of 1-(3-dimethylaminopropyl)-1-(4-fluorophenyl)-1,3-dihydroisobenzofuran-5-carbonitrile
KR20040030609A (ko) * 2001-05-01 2004-04-09 하. 룬트벡 아크티에 셀스카브 경상이성체성 순수 에스시탈로프람의 용도
ES2280892T3 (es) 2001-07-31 2007-09-16 H. Lundbeck A/S Composicion cristalina que contiene escitalopram.
IS7239A (is) * 2001-12-14 2004-04-29 H. Lundbeck A/S Aðferð til framleiðslu á essítalóprami
WO2003057132A2 (en) 2002-01-07 2003-07-17 Sun Pharmaceutical Industries Limited Process for the preparation of 1-[3-(dimethylamino)propyl]-1-(4-fluorophenyl)- 1,3-dihydro-5-isobenzofuran carbonitrile
US7192939B2 (en) * 2002-01-30 2007-03-20 Montana State University Pestalotiopsis microsporia isolates and compounds derived therefrom
CA2381341A1 (en) * 2002-04-09 2003-10-09 Torcan Chemical Ltd. Process and intermediates for preparing escitalopram
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
RS51092B (sr) * 2002-12-23 2010-10-31 H. Lundbeck A/S. Escitalopram bromhidrat i postupak za njegovo pripremanje
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.
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
TWI339651B (en) 2004-02-12 2011-04-01 Lundbeck & Co As H Method for the separation of intermediates which may be used for the preparation of escitalopram
ITMI20040717A1 (it) * 2004-04-09 2004-07-09 Adorkem Technology Spa Procedimento chemo-enzimatico per la preparazione dell'escitalopram
JP2006008603A (ja) * 2004-06-25 2006-01-12 Sumitomo Chemical Co Ltd 光学活性シタロプラムの製造方法、その中間体およびその製造方法
WO2006021971A2 (en) 2004-08-23 2006-03-02 Sun Pharmaceutical Industries Limited 'process for preparation of citalopram and enantiomers'
WO2006090409A1 (en) * 2005-02-28 2006-08-31 Kekule Pharma Ltd., An improved process for the preparation of 5 - carboxyphthalide
GB2442619B (en) * 2005-05-04 2010-05-26 Pharmed Medicare Pvt Ltd Chlorination of sucrose acylates using triphosgene
CN101157674B (zh) * 2005-07-12 2010-04-14 西陇化工股份有限公司 西酞普兰盐的提纯方法
US8258291B2 (en) * 2006-10-25 2012-09-04 Mamtek International Limited Process for the preparation of sucralose by the chlorination of sugar with triphosgene (BTC)
US9339500B2 (en) * 2008-03-04 2016-05-17 Intra-Cellular Therapies, Inc. Methods of treating vasomotor symptoms
US9346777B2 (en) * 2012-09-06 2016-05-24 MediSynergics, LLC Antiprotozoal compounds
US9284291B2 (en) * 2014-07-29 2016-03-15 MediSynergies, LLC Kappa opioid receptor compounds

Family Cites Families (15)

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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
GB8814057D0 (en) * 1988-06-14 1988-07-20 Lundbeck & Co As H New enantiomers & their isolation
DK213290D0 (da) * 1990-09-06 1990-09-06 Lundbeck & Co As H Treatment of cerebrovascular disorders
DE19626659A1 (de) 1996-07-03 1998-01-08 Basf Ag Verfahren zur Herstellung von Phthaliden
DE19627697A1 (de) 1996-07-10 1998-01-15 Basf Ag Verfahren zur Herstellung von Phthaliden
PT1015416E (pt) 1997-07-08 2002-03-28 Lundbeck & Co As H Metodo para a producao de citalopram
UA62985C2 (en) * 1997-11-10 2004-01-15 Lunnbeck As H A method for the preparation of citalopram
AU738359B2 (en) * 1997-11-11 2001-09-13 H. Lundbeck A/S Method for the preparation of citalopram
CA2356188C (en) 1998-12-23 2006-05-23 H. Lundbeck A/S Method for the preparation of 5-cyanophthalide
AR022329A1 (es) 1999-01-29 2002-09-04 Lundbeck & Co As H Metodo para la preparacion de 5-cianoftalida
TR200102957T2 (tr) 1999-04-14 2004-12-21 H. Lundbeck A/S Sitalopram hazırlanması için metod.
ES2169709A1 (es) 1999-10-25 2002-07-01 Lundbeck & Co As H Metodo para la preparacion de citalopram
US6310222B1 (en) 1999-11-01 2001-10-30 Sumika Fine Chemicals Co., Ltd. Production method of 5-phthalancarbonitrile compound, intermediate therefor and production method of the intermediate

Also Published As

Publication number Publication date
DE69904853T2 (de) 2003-09-04
KR100411505B1 (ko) 2003-12-18
NO327038B1 (no) 2009-04-06
DE69904853D1 (de) 2003-02-13
CN1129592C (zh) 2003-12-03
IL142346A0 (en) 2002-03-10
HK1042297B (zh) 2004-09-10
CA2291134C (en) 2006-05-23
CZ20011418A3 (cs) 2001-10-17
NZ510858A (en) 2003-11-28
NO20011936L (no) 2001-06-01
EA002977B1 (ru) 2002-12-26
SK5352001A3 (en) 2002-02-05
BG105457A (en) 2001-12-29
BG64704B1 (bg) 2005-12-30
HU228576B1 (en) 2013-04-29
WO2000023431A1 (en) 2000-04-27
NO20011936D0 (no) 2001-04-19
CA2291134A1 (en) 2000-04-20
AU6326099A (en) 2000-05-08
JP2002527511A (ja) 2002-08-27
ATE230738T1 (de) 2003-01-15
ES2189502T3 (es) 2003-07-01
US6365747B1 (en) 2002-04-02
PL347189A1 (en) 2002-03-25
CN1324351A (zh) 2001-11-28
AU746665B2 (en) 2002-05-02
HUP0104128A2 (hu) 2002-04-29
EP1123284B1 (en) 2003-01-08
HUP0104128A3 (en) 2003-01-28
EP1123284A1 (en) 2001-08-16
IS2256B (is) 2007-06-15
CZ299920B6 (cs) 2008-12-29
HK1042297A1 (en) 2002-08-09
PL199423B1 (pl) 2008-09-30
DK1123284T3 (da) 2003-04-28
BR9915158B1 (pt) 2012-02-22
IS5911A (is) 2001-03-30
BR9915158A (pt) 2001-08-07
AR018693A1 (es) 2001-11-28
SK285719B6 (sk) 2007-07-06
JP3892667B2 (ja) 2007-03-14
KR20010080236A (ko) 2001-08-22

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