HUP0300273A2 - Eljárás 5-szubsztituált 1-(4-fluorfenil)-1,3-dihidroizobenzofurán-származékok lépésenkénti alkilezésére - Google Patents

Eljárás 5-szubsztituált 1-(4-fluorfenil)-1,3-dihidroizobenzofurán-származékok lépésenkénti alkilezésére

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Publication number
HUP0300273A2
HUP0300273A2 HU0300273A HUP0300273A HUP0300273A2 HU P0300273 A2 HUP0300273 A2 HU P0300273A2 HU 0300273 A HU0300273 A HU 0300273A HU P0300273 A HUP0300273 A HU P0300273A HU P0300273 A2 HUP0300273 A2 HU P0300273A2
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HU
Hungary
Prior art keywords
group
hydrogen atom
general formula
formula
alkyl group
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HU0300273A
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English (en)
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Haleh Ahmadian
Hans Petersen
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H. Lundbeck A/S
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Publication date
Application filed by H. Lundbeck A/S filed Critical H. Lundbeck A/S
Publication of HUP0300273A2 publication Critical patent/HUP0300273A2/hu

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D307/00Heterocyclic compounds containing five-membered rings having one oxygen atom as the only ring hetero atom
    • C07D307/77Heterocyclic 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
    • C07D307/87Benzo [c] furans; Hydrogenated benzo [c] furans
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/335Heterocyclic compounds having oxygen as the only ring hetero atom, e.g. fungichromin
    • A61K31/34Heterocyclic 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
    • A61K31/343Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/02Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings not condensed with other rings
    • C07D263/08Heterocyclic 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
    • C07D263/10Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D263/00Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
    • C07D263/52Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/02Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings
    • C07D277/08Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
    • C07D277/10Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D277/00Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings
    • C07D277/60Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings condensed with carbocyclic rings or ring systems
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic 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
    • C07D413/04Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/04Heterocyclic 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Vascular Medicine (AREA)
  • Pain & Pain Management (AREA)
  • Urology & Nephrology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Furan Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyrane Compounds (AREA)

Abstract

A találmány tárgya eljárás á jól ismert antidepresszáns hatásúcitalopram, azaz 1-[3-(dimetilamino)propil]-1-(4-fluorfenil)-1,3-dihidro-5-izobenzofuránkarbonitril előállítására. A találmányértelmében úgy járnak el, hogy valamely (I) általános képletűvegyületet - a képletben R jelentése halogénatom, cianocsoport,hidroxilcsoport, O-triflát-csoport, NHR5 általános képletű csoport(ebben a képletben R5 jelentése hidrogénatom vagy tartalmazóalkilkarbonilcsoport), formilcsoport, CO2R6 vagy CONHR7 általánosképletű csoport (ezekben a képletekben R6 és R7 egymástól függetlenülhidrogénatomot vagy alkilcsoportot jelent) vagy (II) általános képletűoxazolil- vagy tiazolilcsoport (ebben a képletben U jelentése oxigén-vagy kénatom, R1 és R2 egymástól függetlenül hidrogénatomot vagyalkilcsoportot jelent vagy R1 és R2 együtt alkilénláncot alkotnak ésígy spiro-gyűrűt képeznek, R3 jelentése hidrogénatom vagyalkilcsoport, R4 jelentésre hidrogénatom, alkilcsoport,karboxilcsoport vagy az utóbbi valamelyik prekurzorcsoportja, vagy R3és R4 együtt alkilénláncot jelentenek és így spirogyűrűt alkotnak) -reagensek lépésenkénti adagolása útján olyan reagáltatásoknak vetikalá, hogy a citalopram 3-(N,N-dimetilamino)-prop-1-il-szubsztituensekialakuljon, és adott esetben - ha R jelentése cianocsoporttól eltérő- a reakciósorozat egy alkalmas időpontjában R helyettesítőtcianocsoporttá alakítják. Ó
HU0300273A 2000-03-13 2001-03-09 Eljárás 5-szubsztituált 1-(4-fluorfenil)-1,3-dihidroizobenzofurán-származékok lépésenkénti alkilezésére HUP0300273A2 (hu)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DKPA200000403 2000-03-13
DKPA200000414 2000-03-14
PCT/DK2001/000159 WO2001068629A1 (en) 2000-03-13 2001-03-09 Stepwise alkylation of 5-substituted 1-(4-fluorophenyl)-1,3-dihydroisobenzofurans

Publications (1)

Publication Number Publication Date
HUP0300273A2 true HUP0300273A2 (hu) 2003-06-28

Family

ID=26068792

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0300273A HUP0300273A2 (hu) 2000-03-13 2001-03-09 Eljárás 5-szubsztituált 1-(4-fluorfenil)-1,3-dihidroizobenzofurán-származékok lépésenkénti alkilezésére

Country Status (22)

Country Link
US (2) US6864379B2 (hu)
EP (1) EP1265881A1 (hu)
JP (1) JP2003527385A (hu)
KR (1) KR20020080485A (hu)
CN (1) CN1427835A (hu)
AU (1) AU2001239210A1 (hu)
BG (1) BG107046A (hu)
BR (1) BR0109364A (hu)
CA (1) CA2402553A1 (hu)
CZ (1) CZ20023100A3 (hu)
EA (1) EA200200968A1 (hu)
HR (1) HRP20020758A2 (hu)
HU (1) HUP0300273A2 (hu)
IL (1) IL151566A0 (hu)
IS (1) IS6530A (hu)
MX (1) MXPA02008684A (hu)
NO (1) NO20024352L (hu)
NZ (1) NZ521204A (hu)
PL (1) PL357022A1 (hu)
SK (1) SK14522002A3 (hu)
TR (1) TR200202195T2 (hu)
WO (1) WO2001068629A1 (hu)

Families Citing this family (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE237604T1 (de) * 1999-04-14 2003-05-15 Lundbeck & Co As H Verfahren zur herstellung von citalopram
NL1017417C1 (nl) 2000-03-03 2001-03-16 Lundbeck & Co As H Werkwijze voor de bereiding van Citalopram.
NL1017500C1 (nl) 2000-03-13 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van 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
JP2005510518A (ja) * 2001-11-08 2005-04-21 セプラコール, インク. シタロプラムのデスメチル代謝産物及びジデスメチル代謝産物の濃縮された鏡像異性体を用いてうつ病及び他のcns障害を治療する方法
US7078541B2 (en) * 2002-02-07 2006-07-18 Galileo Pharmaceuticals, Inc. Benzofuran derivatives
AR040970A1 (es) 2002-08-12 2005-04-27 Lundbeck & Co As H Metodo para la separacion de intermediarios que pueden ser utilizados para la preparacion de escitalopram
TR200504022T1 (tr) * 2003-03-24 2006-08-21 Hetero Drugs Limited (S)-sitalopram oksalatın yeni sıvı kristal formları.
US20090018351A1 (en) * 2003-11-12 2009-01-15 Dr. Reddy's Laboratories, Inc. Preparation of escitalopram
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
US8615368B2 (en) * 2005-03-10 2013-12-24 Gen-Probe Incorporated Method for determining the amount of an analyte in a sample

Family Cites Families (37)

* 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
ES2148120T3 (es) 1997-07-08 2002-01-16 Lundbeck & Co As H Metodo para la preparacion de citalopram.
UA62985C2 (en) * 1997-11-10 2004-01-15 Lunnbeck As H A method for the preparation of citalopram
ES2149734T3 (es) 1997-11-11 2003-02-16 Lundbeck & Co As H Metodo para la preparacion de citalopram.
CN1129592C (zh) 1998-10-20 2003-12-03 H·隆德贝克有限公司 制备西酞普兰的方法
SI1140886T1 (en) 1998-12-23 2003-08-31 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
ATE237604T1 (de) 1999-04-14 2003-05-15 Lundbeck & Co As H Verfahren zur herstellung von citalopram
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
EP1228056B1 (en) 1999-10-25 2004-09-22 H. Lundbeck A/S 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.
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
EA004742B1 (ru) * 1999-12-28 2004-08-26 Х.Лундбекк А/С Способ получения циталопрама
JP2003519218A (ja) * 1999-12-30 2003-06-17 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
SI1254129T1 (en) 2000-01-14 2004-02-29 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.
US6433196B1 (en) 2000-02-17 2002-08-13 Sumika Fine Chemicals Co., Ltd. Production method of citalopram, intermediate therefor and production method of the intermediate
IES20010143A2 (en) * 2000-02-24 2001-07-25 Lundbeck & Co As H Method for the preparation of citalopram
NL1017415C1 (nl) 2000-02-24 2001-05-18 Lundbeck & Co As H Werkwijze voor de bereiding van 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
CN1429219A (zh) * 2000-03-13 2003-07-09 H·隆德贝克有限公司 制备西酞普兰的方法
NL1017500C1 (nl) * 2000-03-13 2001-04-26 Lundbeck & Co As H Werkwijze voor de bereiding van Citalopram.
WO2001068630A1 (en) * 2000-03-14 2001-09-20 H. Lundbeck A/S 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
BR0106976A (pt) 2000-07-06 2002-07-23 Lundbeck & Co As H Método para a preparação de citalopram
IL144816A (en) 2000-08-18 2005-09-25 Lundbeck & Co As H Method for the preparation of citalopram
SG167655A1 (en) 2000-12-22 2011-01-28 Lundbeck & Co As H Method for the preparation of pure 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

Also Published As

Publication number Publication date
EA200200968A1 (ru) 2003-02-27
IS6530A (is) 2002-08-27
IL151566A0 (en) 2003-04-10
PL357022A1 (en) 2004-07-12
US6864379B2 (en) 2005-03-08
NO20024352L (no) 2002-10-08
NO20024352D0 (no) 2002-09-12
HRP20020758A2 (en) 2004-12-31
CN1427835A (zh) 2003-07-02
WO2001068629A1 (en) 2001-09-20
CA2402553A1 (en) 2001-09-20
KR20020080485A (ko) 2002-10-23
MXPA02008684A (es) 2003-02-24
JP2003527385A (ja) 2003-09-16
AU2001239210A1 (en) 2001-09-24
US20050020670A1 (en) 2005-01-27
BG107046A (en) 2003-05-30
US20030083509A1 (en) 2003-05-01
CZ20023100A3 (cs) 2003-02-12
BR0109364A (pt) 2002-12-24
EP1265881A1 (en) 2002-12-18
TR200202195T2 (tr) 2002-12-23
SK14522002A3 (sk) 2003-03-04
NZ521204A (en) 2004-03-26

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