BG105457A - Метод за получаване на циталопрам - Google Patents

Метод за получаване на циталопрам

Info

Publication number
BG105457A
BG105457A BG105457A BG10545701A BG105457A BG 105457 A BG105457 A BG 105457A BG 105457 A BG105457 A BG 105457A BG 10545701 A BG10545701 A BG 10545701A BG 105457 A BG105457 A BG 105457A
Authority
BG
Bulgaria
Prior art keywords
citalopram
alkyl
preparation
hydrogen
ring
Prior art date
Application number
BG105457A
Other languages
English (en)
Other versions
BG64704B1 (bg
Inventor
Leone Dall'asta
Umberto Casazza
Hans Petersen
Original Assignee
H.Lundbeck A/S
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 IT98MI002242 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 H.Lundbeck A/S filed Critical H.Lundbeck A/S
Publication of BG105457A publication Critical patent/BG105457A/bg
Publication of BG64704B1 publication Critical patent/BG64704B1/bg

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

Abstract

Изобретението се отнася до метод за получаване нациталопрам или всеки от неговите енантиомери и техните присъединителни с киселина соли. По метода се третира съединение с формула@@в която Х е О или S; R1-R2 са поотделно независимо избрани от водород и С1-6 алкил, или R1 и R2 заедно образуват С2-5 алкиленова верига и по този начин формират спиро-пръстен; R3 е избран от водород и С1-6 алкил, R4 е избран от водород, С1-6 алкил, карбоксигрупа или нейна прекурсорна група, или R3 и R4 заедно образуват С2-5 алкиленова верига и по този начин формиратспиропръстен, с дехидратиращо средство или в даден случай, когато Х е S, тиазолиновият пръстен се разцепва термично или се третира в присъствието на радикалов инициатор до получаване на циталопрам. Изобретението се отнася също до междинни съединения, използвани в новия метод за получаване на циталопрам, както и до циталопрам, получен по новия метод.
BG105457A 1998-10-20 2001-04-20 Метод за получаване на циталопрам BG64704B1 (bg)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
IT98MI002242 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.

Publications (2)

Publication Number Publication Date
BG105457A true BG105457A (bg) 2001-12-29
BG64704B1 BG64704B1 (bg) 2005-12-30

Family

ID=27274104

Family Applications (1)

Application Number Title Priority Date Filing Date
BG105457A BG64704B1 (bg) 1998-10-20 2001-04-20 Метод за получаване на циталопрам

Country Status (25)

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

Families Citing this family (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN1149208C (zh) 1998-12-23 2004-05-12 H.隆德贝克有限公司 制备5-氰基2-苯并[c]呋喃酮的方法
AR022329A1 (es) 1999-01-29 2002-09-04 Lundbeck & Co As H Metodo para la preparacion de 5-cianoftalida
CN1142926C (zh) 1999-04-14 2004-03-24 H·隆德贝克有限公司 制备西酞普兰的方法
ITMI991581A1 (it) * 1999-06-25 2001-01-15 Lundbeck & Co As H Metodo per la preparazione di citalopram
ITMI991579A1 (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
NZ512406A (en) 1999-10-25 2004-01-30 H Method for the preparation of citalopram
ES2169709A1 (es) 1999-10-25 2002-07-01 Lundbeck & Co As H Metodo para la preparacion de citalopram
AR026063A1 (es) * 1999-11-01 2002-12-26 Lundbeck & Co As H Metodo para la preparacion de 5-carboxiftalida.
CZ20022213A3 (cs) 1999-12-28 2002-09-11 H. Lundbeck A/S Způsob výroby citalopramu
SI1246813T1 (en) 1999-12-30 2004-08-31 H. Lundbeck A/S Method for the preparation of citalopram
CZ20022601A3 (cs) * 2000-01-14 2002-10-16 H. Lundbeck A/S Způsob výroby 5-kyanoftalidu
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
NL1017417C1 (nl) 2000-03-03 2001-03-16 Lundbeck & Co As H Werkwijze voor de bereiding van Citalopram.
GB0005477D0 (en) * 2000-03-07 2000-04-26 Resolution Chemicals Limited Process for the preparation of citalopram
EA200200968A1 (ru) * 2000-03-13 2003-02-27 Х.Лундбекк А/С Поэтапное алкилирование 5-замещенных 1-(4-фторфенил)-1,3-дигидроизобензофуранов
NL1017500C1 (nl) 2000-03-13 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van Citalopram.
MXPA02008869A (es) 2000-03-13 2003-02-10 Lundbeck & Co As H Metodo para la preparacion de citalopram.
GB2357762B (en) * 2000-03-13 2002-01-30 Lundbeck & Co As H Crystalline base of citalopram
JP2003527386A (ja) 2000-03-14 2003-09-16 ハー・ルンドベック・アクチエゼルスカベット シタロプラムの製造方法
AU2001244086A1 (en) * 2000-03-16 2001-09-24 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
ES2228824T3 (es) * 2000-12-22 2005-04-16 H. Lundbeck A/S Metodo de preparacion de citalopram puro.
IL147162A0 (en) 2000-12-28 2002-08-14 Lundbeck & Co As H Process for the preparation of pure citalopram
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
CA2445843A1 (en) * 2001-05-01 2002-11-07 H. Lundbeck A/S The use of enantiomeric pure escitalopram
UA79930C2 (en) 2001-07-31 2007-08-10 Lundbeck & Co As H Crystalline composition containing escitalopram
IS7239A (is) * 2001-12-14 2004-04-29 H. Lundbeck A/S Aðferð til framleiðslu á essítalóprami
US7148364B2 (en) 2002-01-07 2006-12-12 Sun Pharmaceutical Industries 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
WO2004056791A1 (en) * 2002-12-23 2004-07-08 H. Lundbeck A/S Escitalopram hydrobromide and a method for the preparation thereof
US7019153B2 (en) 2003-06-10 2006-03-28 Sun Pharmaceutical Industries Limited Process for hydrogenolysis of [1-(3-dimethylamino)propyl)]-1-(4-fluorophenyl)-1,3-dihydro-5-halo-isobenzofuran acetamido-3-substituted-3-cephem-4-carboxylic acid
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
EP2141156A1 (en) 2004-08-23 2010-01-06 Sun Pharma Global FZE 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

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GB1143702A (bg) 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
EP1015416B1 (en) * 1997-07-08 2001-09-19 H. Lundbeck A/S Method for the preparation of citalopram
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CN1149208C (zh) 1998-12-23 2004-05-12 H.隆德贝克有限公司 制备5-氰基2-苯并[c]呋喃酮的方法
AR022329A1 (es) 1999-01-29 2002-09-04 Lundbeck & Co As H Metodo para la preparacion de 5-cianoftalida
CN1142926C (zh) 1999-04-14 2004-03-24 H·隆德贝克有限公司 制备西酞普兰的方法
ES2169709A1 (es) 1999-10-25 2002-07-01 Lundbeck & Co As H Metodo para la preparacion de citalopram
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Also Published As

Publication number Publication date
BG64704B1 (bg) 2005-12-30
HU228576B1 (en) 2013-04-29
CN1324351A (zh) 2001-11-28
SK285719B6 (sk) 2007-07-06
NO20011936L (no) 2001-06-01
CA2291134A1 (en) 2000-04-20
JP2002527511A (ja) 2002-08-27
ES2189502T3 (es) 2003-07-01
AR018693A1 (es) 2001-11-28
ATE230738T1 (de) 2003-01-15
DK1123284T3 (da) 2003-04-28
HK1042297B (zh) 2004-09-10
PL199423B1 (pl) 2008-09-30
KR100411505B1 (ko) 2003-12-18
JP3892667B2 (ja) 2007-03-14
SK5352001A3 (en) 2002-02-05
HUP0104128A3 (en) 2003-01-28
EP1123284A1 (en) 2001-08-16
CN1129592C (zh) 2003-12-03
CZ20011418A3 (cs) 2001-10-17
PL347189A1 (en) 2002-03-25
EA200100457A1 (ru) 2001-10-22
NO327038B1 (no) 2009-04-06
NO20011936D0 (no) 2001-04-19
IS2256B (is) 2007-06-15
NZ510858A (en) 2003-11-28
AU6326099A (en) 2000-05-08
IL142346A0 (en) 2002-03-10
DE69904853T2 (de) 2003-09-04
IS5911A (is) 2001-03-30
HK1042297A1 (en) 2002-08-09
WO2000023431A1 (en) 2000-04-27
CZ299920B6 (cs) 2008-12-29
BR9915158A (pt) 2001-08-07
HUP0104128A2 (hu) 2002-04-29
BR9915158B1 (pt) 2012-02-22
EA002977B1 (ru) 2002-12-26
CA2291134C (en) 2006-05-23
DE69904853D1 (de) 2003-02-13
US6365747B1 (en) 2002-04-02
EP1123284B1 (en) 2003-01-08
AU746665B2 (en) 2002-05-02
KR20010080236A (ko) 2001-08-22

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