EA200000102A1 - Способ получения циталопрама - Google Patents

Способ получения циталопрама

Info

Publication number
EA200000102A1
EA200000102A1 EA200000102A EA200000102A EA200000102A1 EA 200000102 A1 EA200000102 A1 EA 200000102A1 EA 200000102 A EA200000102 A EA 200000102A EA 200000102 A EA200000102 A EA 200000102A EA 200000102 A1 EA200000102 A1 EA 200000102A1
Authority
EA
Eurasian Patent Office
Prior art keywords
formula
cytaloprama
obtaining
compound
citalopram
Prior art date
Application number
EA200000102A
Other languages
English (en)
Other versions
EA001728B1 (ru
Inventor
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
Application filed by Х.Лундбекк А/С filed Critical Х.Лундбекк А/С
Publication of EA200000102A1 publication Critical patent/EA200000102A1/ru
Publication of EA001728B1 publication Critical patent/EA001728B1/ru

Links

Classifications

    • 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
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/335—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide
    • A61K31/343—Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin having five-membered rings with one oxygen as the only ring hetero atom, e.g. isosorbide condensed with a carbocyclic ring, e.g. coumaran, bufuralol, befunolol, clobenfurol, amiodarone
    • 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
    • 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
    • C07C229/00—Compounds containing amino and carboxyl groups bound to the same carbon skeleton
    • C07C229/38—Compounds containing amino and carboxyl groups bound to the same carbon skeleton having amino groups bound to acyclic carbon atoms and carboxyl groups bound to carbon atoms of six-membered aromatic rings of the same carbon skeleton
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C235/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms
    • C07C235/70—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton
    • C07C235/84—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by oxygen atoms having carbon atoms of carboxamide groups and doubly-bound oxygen atoms bound to the same carbon skeleton with the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a six-membered aromatic ring
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07C—ACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C237/00—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups
    • C07C237/28—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton
    • C07C237/30—Carboxylic acid amides, the carbon skeleton of the acid part being further substituted by amino groups having the carbon atom of at least one of the carboxamide groups bound to a carbon atom of a non-condensed six-membered aromatic ring of the carbon skeleton having the nitrogen atom of the carboxamide group bound to hydrogen atoms or to acyclic carbon atoms
    • 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)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Epidemiology (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)
  • Furan Compounds (AREA)

Abstract

Способ получения циталопрама, включающий стадии взаимодействия соединения формулы (IV)где Rпредставляет Cалкил, и Х представляет O или NH, последовательно с реактивом Гриньяра 4-галогенфторфенила и реактивом Гриньяра 3-галоген-N,N-диметилпропиламина, соответственно, осуществления замыкания кольца в полученном соединении формулы (V)где Rи X являются такими, как определено выше, и превращения полученного 1,3-дигидроизобензофуранового соединения в соответствующее 5-цианопроизводное, то есть циталопрам.Международная заявка была опубликована вместе с отчетом о международном поиске.
EA200000102A 1997-07-08 1998-03-03 Способ получения циталопрама EA001728B1 (ru)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US5278897P 1997-07-08 1997-07-08
DK82697 1997-07-08
PCT/DK1998/000081 WO1998019513A2 (en) 1997-07-08 1998-03-03 Method for the preparation of citalopram

Publications (2)

Publication Number Publication Date
EA200000102A1 true EA200000102A1 (ru) 2000-06-26
EA001728B1 EA001728B1 (ru) 2001-08-27

Family

ID=26064729

Family Applications (1)

Application Number Title Priority Date Filing Date
EA200000102A EA001728B1 (ru) 1997-07-08 1998-03-03 Способ получения циталопрама

Country Status (23)

Country Link
US (1) US6229026B1 (ru)
EP (1) EP1015416B1 (ru)
JP (1) JP3526581B2 (ru)
KR (1) KR100357975B1 (ru)
CN (1) CN1206207C (ru)
AT (1) ATE205824T1 (ru)
AU (1) AU737610B2 (ru)
BG (1) BG64823B1 (ru)
CA (1) CA2291067C (ru)
CZ (1) CZ291440B6 (ru)
DE (2) DE1015416T1 (ru)
DK (1) DK1015416T3 (ru)
EA (1) EA001728B1 (ru)
ES (1) ES2148120T3 (ru)
HU (1) HU228744B1 (ru)
IL (2) IL133511A (ru)
IS (1) IS2023B (ru)
NO (1) NO322146B1 (ru)
NZ (1) NZ501737A (ru)
PT (1) PT1015416E (ru)
SK (1) SK283309B6 (ru)
TR (1) TR200000066T2 (ru)
WO (1) WO1998019513A2 (ru)

Families Citing this family (52)

* 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
CA2291134C (en) 1998-10-20 2006-05-23 H. Lundbeck A/S Method for the preparation of citalopram
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
AU759716B2 (en) * 1999-04-14 2003-04-17 H. Lundbeck A/S 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
CH692298A5 (de) 1999-10-25 2002-04-30 Lundbeck & Co As H Verfahren zur Herstellung von Zwischenstufen für die Citalopramsynthese sowie zur Herstellung von Escitalopram.
TR200401456T1 (tr) * 1999-10-25 2005-04-21 H. Lundbeck A/S Sitalopram hazırlanması için yöntem.
AR026063A1 (es) 1999-11-01 2002-12-26 Lundbeck & Co As H Metodo para la preparacion de 5-carboxiftalida.
EA004742B1 (ru) 1999-12-28 2004-08-26 Х.Лундбекк А/С Способ получения циталопрама
BR9917604A (pt) 1999-12-30 2002-12-31 Lundbeck & Co As H Método para preparação de citalopram
HUP0300343A2 (hu) 2000-01-14 2003-06-28 H. Lundbeck A/S Eljárás 5-cianoftalid előállítására
IT1317729B1 (it) * 2000-01-18 2003-07-15 Norpharma S P A Procedimento per la preparazione della 5-carbossiftalide.
NL1017415C1 (nl) 2000-02-24 2001-05-18 Lundbeck & Co As H Werkwijze voor de bereiding van 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
GB2357762B (en) 2000-03-13 2002-01-30 Lundbeck & Co As H Crystalline base of citalopram
NL1017500C1 (nl) 2000-03-13 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van 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
PL360110A1 (en) 2000-03-13 2004-09-06 H.Lundbeck A/S Method for the preparation of citalopram
TR200202155T2 (tr) 2000-03-14 2002-12-23 H. Lundbeck A/S Sitalopramin preparasyon metodu
CZ20023406A3 (cs) * 2000-03-16 2003-01-15 H. Lundbeck A/S Způsob výroby 5-kyano-1-(4-fluorfenyl)-1,3-dihydroisobenzofuranu
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
CA2354877C (en) * 2000-08-18 2006-05-02 H. Lundbeck A/S 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.
NL1017525C1 (nl) * 2000-12-22 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van zuiver Citalopram
ATE222899T1 (de) * 2000-12-28 2002-09-15 Lundbeck & Co As H Verfahren zur herstellung von reinem citalopram
DE10112828C1 (de) * 2000-12-28 2002-11-21 Lundbeck & Co As H Verfahren zur Herstellung von 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
BG65271B1 (bg) * 2001-06-18 2007-11-30 H. Lundbeck A/S Метод за получаване на циталопрам
IN192057B (ru) * 2001-07-19 2004-02-14 Ranbaxy Lab Ltd
BR0206164A (pt) 2001-07-31 2003-10-28 Lundbeck & Co As H Partìculas cristalinas de oxalato de escitalopram, método para a produção de partìculas cristalinas de oxalato de escitalopram, e, forma de dosagem unitária sólida
DE60108105T2 (de) * 2001-08-02 2005-12-08 Infosint Sa Verfahren zur Herstellung von 5-substituierten Isobenzofuranen
GR1004635B (el) * 2001-08-14 2004-07-14 H@Αlundbeckαa@Sαα Μεθοδοσαπαρασκευησατησασιταλοπραμης@αα
EP1288211A1 (en) * 2001-08-28 2003-03-05 Sekhsaria Chemicals Ltd. Improved process for the manufacture of citalopram hydrobromide from 5-bromophthalide
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
GB2387844B (en) * 2002-02-27 2005-05-11 Matrix Lab Ltd Separation of impurities from a crude mixture of citalopram
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
AU2002330730A1 (en) * 2002-08-14 2004-03-03 Natco Pharma Limited Process for the preparation of high purity citalopram and its pharmaceutically acceptable salts
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.
US7687645B2 (en) 2003-03-21 2010-03-30 H. Lundbeck A/S Intermediates for the preparation of citalopram and escitalopram
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
ES2240931T3 (es) * 2003-10-28 2005-10-16 Adorkem Technology Spa Procedimiento para la preparacion de citalopram.
US7790935B2 (en) 2004-08-23 2010-09-07 Sun Pharma Global Fze Process for preparation of citalopram and enantiomers
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
US9339500B2 (en) * 2008-03-04 2016-05-17 Intra-Cellular Therapies, Inc. Methods of treating vasomotor symptoms

Family Cites Families (5)

* Cited by examiner, † Cited by third party
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
DK213290D0 (da) * 1990-09-06 1990-09-06 Lundbeck & Co As H Treatment of cerebrovascular disorders
NZ243065A (en) 1991-06-13 1995-07-26 Lundbeck & Co As H Piperidine derivatives and pharmaceutical compositions

Also Published As

Publication number Publication date
JP2002509526A (ja) 2002-03-26
AU737610B2 (en) 2001-08-23
CZ200062A3 (cs) 2000-07-12
DK1015416T3 (da) 2001-11-05
EP1015416A2 (en) 2000-07-05
NZ501737A (en) 2001-10-26
IL133511A (en) 2004-05-12
CA2291067C (en) 2002-07-30
NO322146B1 (no) 2006-08-21
DE69801764T2 (de) 2002-07-04
IS2023B (is) 2005-08-15
ES2148120T1 (es) 2000-10-16
PT1015416E (pt) 2002-03-28
BG64823B1 (bg) 2006-05-31
IL153125A (en) 2008-11-03
US6229026B1 (en) 2001-05-08
WO1998019513A3 (en) 2000-05-04
EP1015416B1 (en) 2001-09-19
IS5300A (is) 1999-12-14
DE69801764D1 (de) 2001-10-25
CA2291067A1 (en) 1998-05-14
WO1998019513A2 (en) 1998-05-14
SK32000A3 (en) 2000-07-11
AU6609898A (en) 1998-05-29
ATE205824T1 (de) 2001-10-15
CN1495157A (zh) 2004-05-12
IL133511A0 (en) 2001-04-30
CN1206207C (zh) 2005-06-15
BG104116A (en) 2000-12-29
KR100357975B1 (ko) 2002-10-25
JP3526581B2 (ja) 2004-05-17
DE1015416T1 (de) 2000-10-05
HUP0003177A3 (en) 2002-12-28
CZ291440B6 (cs) 2003-03-12
TR200000066T2 (tr) 2000-11-21
SK283309B6 (sk) 2003-05-02
KR20010021516A (ko) 2001-03-15
HUP0003177A2 (hu) 2001-04-28
EA001728B1 (ru) 2001-08-27
ES2148120T3 (es) 2002-01-16
NO20000008L (no) 2000-01-03
HU228744B1 (en) 2013-05-28
NO20000008D0 (no) 2000-01-03

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Legal Events

Date Code Title Description
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

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): BY RU