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) DE69801764T2 (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
WO2000023431A1 (en) * 1998-10-20 2000-04-27 H. Lundbeck A/S Method for the preparation of citalopram
HK1043130B (zh) * 1998-12-23 2005-03-04 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
IL145615A0 (en) 1999-04-14 2002-06-30 Lundbeck & Co As 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
HK1043129B (zh) 1999-10-25 2004-10-21 H‧隆德贝克有限公司 西酞普蘭的製備方法
GB2360281B (en) 1999-10-25 2002-01-16 Lundbeck & Co As H Method for the preparation of citalopram
AR026063A1 (es) 1999-11-01 2002-12-26 Lundbeck & Co As H Metodo para la preparacion de 5-carboxiftalida.
NZ519739A (en) 1999-12-28 2004-03-26 H Method for the preparation of citalopram
PT1246813E (pt) * 1999-12-30 2004-02-27 Lundbeck & Co As H Metodo para a preparacao de citalopram
WO2001051477A1 (en) 2000-01-14 2001-07-19 H. Lundbeck A/S Method for the preparation of 5-cyanophthalide
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
NL1017500C1 (nl) 2000-03-13 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van Citalopram.
BR0109364A (pt) 2000-03-13 2002-12-24 Lundbeck & Co As H Métodos para fabricação de citalopram através de alquilação escalonada de 5-substituìda 1- (4-fluorofenil) - 1,3- diidroisobenzofuranos e citalopram
SK14602002A3 (sk) 2000-03-13 2003-02-04 H. Lundbeck A/S Spôsob výroby citalopramu a medziprodukty
GB2357762B (en) * 2000-03-13 2002-01-30 Lundbeck & Co As H Crystalline base of citalopram
IL151488A0 (en) 2000-03-14 2003-04-10 Lundbeck & Co As H Method for the preparation of citalopram
TR200202168T2 (tr) * 2000-03-16 2002-12-23 H. Lundbeck A/S 5-Siyano-1-(4-Florofenil)-1,3-Dihidroizobenzofuranların preparasyon metodu
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
IL144816A (en) * 2000-08-18 2005-09-25 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.
TR200201166T1 (tr) * 2000-12-22 2002-10-21 H.Lundbecks A/S Saf sitalopram hazırlanması için yöntem
DE10112828C1 (de) * 2000-12-28 2002-11-21 Lundbeck & Co As H Verfahren zur Herstellung von Citalopram
JP2003519121A (ja) * 2000-12-28 2003-06-17 ハー・ルンドベック・アクチエゼルスカベット 純粋なシタロプラムの製造方法
CA2435925A1 (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
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
ATE352546T1 (de) 2001-07-31 2007-02-15 Lundbeck & Co As H Kristalline zusammensetzung enthaltend escitalopram
DK1281707T3 (da) * 2001-08-02 2005-05-02 Infosint Sa Fremgangsmåde til fremstilling af 5-substituerede isobenzenfuraner
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
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
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
WO2004016602A1 (en) * 2002-08-14 2004-02-26 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.
EP1611118A2 (en) 2003-03-21 2006-01-04 H. Lundbeck A/S Intermediates for the preparation of citalopram and escitalopram
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.
PT1506963E (pt) * 2003-10-28 2005-08-31 Adorkem Technology Spa Processo para a preparacao de citalopram
KR101166280B1 (ko) 2004-08-23 2013-11-27 썬 파마 글로벌 에프제트이 시탈로프램 및 에난티오머의 제조 방법
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
WO2009111031A2 (en) * 2008-03-04 2009-09-11 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
GB1143703A (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
JP3526581B2 (ja) 2004-05-17
WO1998019513A3 (en) 2000-05-04
EA001728B1 (ru) 2001-08-27
NO322146B1 (no) 2006-08-21
IL153125A (en) 2008-11-03
EP1015416A2 (en) 2000-07-05
AU6609898A (en) 1998-05-29
DE1015416T1 (de) 2000-10-05
ATE205824T1 (de) 2001-10-15
CA2291067A1 (en) 1998-05-14
ES2148120T3 (es) 2002-01-16
WO1998019513A2 (en) 1998-05-14
JP2002509526A (ja) 2002-03-26
DE69801764D1 (de) 2001-10-25
IS2023B (is) 2005-08-15
BG104116A (en) 2000-12-29
CZ291440B6 (cs) 2003-03-12
BG64823B1 (bg) 2006-05-31
HU228744B1 (en) 2013-05-28
TR200000066T2 (tr) 2000-11-21
IL133511A0 (en) 2001-04-30
NO20000008L (no) 2000-01-03
AU737610B2 (en) 2001-08-23
KR20010021516A (ko) 2001-03-15
SK283309B6 (sk) 2003-05-02
SK32000A3 (en) 2000-07-11
US6229026B1 (en) 2001-05-08
CN1495157A (zh) 2004-05-12
NZ501737A (en) 2001-10-26
HUP0003177A2 (hu) 2001-04-28
EP1015416B1 (en) 2001-09-19
IS5300A (is) 1999-12-14
CA2291067C (en) 2002-07-30
CZ200062A3 (cs) 2000-07-12
IL133511A (en) 2004-05-12
ES2148120T1 (es) 2000-10-16
DE69801764T2 (de) 2002-07-04
DK1015416T3 (da) 2001-11-05
PT1015416E (pt) 2002-03-28
HUP0003177A3 (en) 2002-12-28
CN1206207C (zh) 2005-06-15
KR100357975B1 (ko) 2002-10-25
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