HUP0203635A2 - Eljárás citalopram előállítására - Google Patents

Eljárás citalopram előállítására

Info

Publication number
HUP0203635A2
HUP0203635A2 HU0203635A HUP0203635A HUP0203635A2 HU P0203635 A2 HUP0203635 A2 HU P0203635A2 HU 0203635 A HU0203635 A HU 0203635A HU P0203635 A HUP0203635 A HU P0203635A HU P0203635 A2 HUP0203635 A2 HU P0203635A2
Authority
HU
Hungary
Prior art keywords
formula
compound
converted
citalopram
group
Prior art date
Application number
HU0203635A
Other languages
English (en)
Inventor
Jakob Felding
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
Application filed by H. Lundbeck A/S filed Critical H. Lundbeck A/S
Publication of HUP0203635A2 publication Critical patent/HUP0203635A2/hu
Publication of HUP0203635A3 publication Critical patent/HUP0203635A3/hu

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
    • 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
    • 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
    • C07C215/02—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton
    • C07C215/22—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated
    • C07C215/28—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings
    • C07C215/34—Compounds containing amino and hydroxy groups bound to the same carbon skeleton having hydroxy groups and amino groups bound to acyclic carbon atoms of the same carbon skeleton the carbon skeleton being unsaturated and containing six-membered aromatic rings containing hydroxy groups and carbon atoms of six-membered aromatic rings bound to the same carbon atom of the carbon skeleton and at least one hydroxy group bound to another carbon atom of the 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
    • C07D307/02—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings
    • C07D307/26—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D307/28—Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom 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
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)

Abstract

A találmány tárgya eljárás a jól ismert antidepresszáns hatásúcitalopram, azaz 1-[3-(dimetilamino)propil]-1-(4-fluorfenil)-1,3-dihidro-5-izobenzofuránkarbonitril előállítására. A találmányértelmében úgy járnak el, hogy (II) képletű vegyületet a) valamely(III) általános képletű diénnel - a képletben X jelentése oxigén- vagykénatom vagy SO2, -N=N-, -CO-O- vagy -O-CO- képletű csoport -reagáltatják, majd oxidálást végeznek, vagy pedig b) valamely (IV)általános képletű vegyülettel - a képletben R jelentése alkilcsoport,adott esetben szubsztituált arilcsoport vagy adott esetbenszubsztituált aralkilcsoport - reagáltatják, majd egy így kapott (V)általános képletű vegyületet - a képletben R jelentése a korábbanmegadott - a (VI) képletű vegyületté alakítják, a (VI) képletűvegyületet a (VII) képletű vegyületté alakítják és végül a (VII)képletű vegyületet oxidálják; és kívánt esetben a szabad bázis vagysavaddíciós só formájában kapott citalopramot gyógyászatilagelfogadható sóvá alakítják. A találmány továbbá az eljárás soránhasznosított új köztitermékekre vonatkozik. Ó
HU0203635A 1999-12-28 1999-12-28 Method for the preparation of citalopram HUP0203635A3 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
PCT/DK1999/000739 WO2001047909A1 (en) 1999-12-28 1999-12-28 Method for the preparation of citalopram

Publications (2)

Publication Number Publication Date
HUP0203635A2 true HUP0203635A2 (hu) 2003-02-28
HUP0203635A3 HUP0203635A3 (en) 2005-02-28

Family

ID=8157173

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0203635A HUP0203635A3 (en) 1999-12-28 1999-12-28 Method for the preparation of citalopram

Country Status (26)

Country Link
US (1) US6762307B2 (hu)
EP (1) EP1246812B1 (hu)
JP (1) JP2003519136A (hu)
KR (1) KR20020073489A (hu)
CN (1) CN1398263A (hu)
AT (1) ATE261953T1 (hu)
AU (1) AU778751B2 (hu)
BG (1) BG106939A (hu)
CA (1) CA2395404A1 (hu)
CZ (1) CZ20022213A3 (hu)
DE (1) DE69915713T2 (hu)
DK (1) DK1246812T3 (hu)
EA (1) EA004742B1 (hu)
ES (1) ES2219095T3 (hu)
HU (1) HUP0203635A3 (hu)
IL (1) IL150335A0 (hu)
IS (1) IS6435A (hu)
MX (1) MXPA02006503A (hu)
NO (1) NO20023126D0 (hu)
NZ (1) NZ519739A (hu)
PL (1) PL355532A1 (hu)
PT (1) PT1246812E (hu)
SI (1) SI1246812T1 (hu)
SK (1) SK9282002A3 (hu)
TR (1) TR200201678T2 (hu)
WO (1) WO2001047909A1 (hu)

Families Citing this family (16)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TR200102957T2 (tr) 1999-04-14 2004-12-21 H. Lundbeck A/S Sitalopram hazırlanması için metod.
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
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
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
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
ATE257832T1 (de) 2000-03-14 2004-01-15 Lundbeck & Co As H Verfahren zur herstellung von citalopram
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
US20050154052A1 (en) * 2003-03-24 2005-07-14 Hetero Drugs Limited Novel crystalline forms of (s)-citalopram oxalate
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
US20090247772A1 (en) * 2005-11-14 2009-10-01 H. Lundbeck A/S Method for the Preparation of Escitalopram
WO2009147687A2 (en) * 2008-06-03 2009-12-10 Shodhana Laboratories Limited An improved process for the separation of enantiomerically pure compounds
US20110092719A1 (en) * 2008-06-16 2011-04-21 Shodhana Laboratories Limited Preparation of Escitalopram, Its Salts and Intermediates

Family Cites Families (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB1143702A (hu) 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
US5296507A (en) 1990-09-06 1994-03-22 H.Lundbeck A/S Treatment of cerbrovascular 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
HU228576B1 (en) 1998-10-20 2013-04-29 Lundbeck & Co As H 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.
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
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
AR026063A1 (es) 1999-11-01 2002-12-26 Lundbeck & Co As H Metodo para la preparacion de 5-carboxiftalida.
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
IES20010143A2 (en) 2000-02-24 2001-07-25 Lundbeck & Co As H Method for the preparation of citalopram
FR2805812A1 (fr) 2000-02-24 2001-09-07 Lundbeck & Co As H Procede de preparation du citalopram
GB0005477D0 (en) 2000-03-07 2000-04-26 Resolution Chemicals Limited Process for the preparation of citalopram
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

Also Published As

Publication number Publication date
IS6435A (is) 2002-06-19
IL150335A0 (en) 2002-12-01
EA004742B1 (ru) 2004-08-26
EP1246812B1 (en) 2004-03-17
AU1858300A (en) 2001-07-09
CA2395404A1 (en) 2001-07-05
NO20023126L (no) 2002-06-27
SI1246812T1 (en) 2004-08-31
DE69915713T2 (de) 2005-03-03
CZ20022213A3 (cs) 2002-09-11
PL355532A1 (en) 2004-05-04
CN1398263A (zh) 2003-02-19
DE69915713D1 (de) 2004-04-22
DK1246812T3 (da) 2004-07-05
ES2219095T3 (es) 2004-11-16
US20030060641A1 (en) 2003-03-27
MXPA02006503A (es) 2002-12-09
KR20020073489A (ko) 2002-09-26
ATE261953T1 (de) 2004-04-15
NZ519739A (en) 2004-03-26
EP1246812A1 (en) 2002-10-09
NO20023126D0 (no) 2002-06-27
EA200200719A1 (ru) 2002-12-26
US6762307B2 (en) 2004-07-13
AU778751B2 (en) 2004-12-16
WO2001047909A1 (en) 2001-07-05
BG106939A (en) 2003-03-31
HUP0203635A3 (en) 2005-02-28
JP2003519136A (ja) 2003-06-17
SK9282002A3 (en) 2002-11-06
PT1246812E (pt) 2004-08-31
TR200201678T2 (tr) 2002-10-21

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