WO2001002383A8 - Process for the synthesis of citalopram - Google Patents

Process for the synthesis of citalopram

Info

Publication number
WO2001002383A8
WO2001002383A8 PCT/EP2000/006426 EP0006426W WO0102383A8 WO 2001002383 A8 WO2001002383 A8 WO 2001002383A8 EP 0006426 W EP0006426 W EP 0006426W WO 0102383 A8 WO0102383 A8 WO 0102383A8
Authority
WO
WIPO (PCT)
Prior art keywords
citalopram
synthesis
converted
halophthalane
hydrazone
Prior art date
Application number
PCT/EP2000/006426
Other languages
French (fr)
Other versions
WO2001002383A3 (en
WO2001002383A2 (en
Inventor
Eva Bolzonella
Andrea Castellin
Andrea Nicole
Original Assignee
Lundbeck Pharmaceuticals Italy
Eva Bolzonella
Andrea Castellin
Andrea Nicole
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 Lundbeck Pharmaceuticals Italy, Eva Bolzonella, Andrea Castellin, Andrea Nicole filed Critical Lundbeck Pharmaceuticals Italy
Priority to AU64328/00A priority Critical patent/AU6432800A/en
Publication of WO2001002383A2 publication Critical patent/WO2001002383A2/en
Publication of WO2001002383A3 publication Critical patent/WO2001002383A3/en
Priority to EA200200332A priority patent/EA200200332A1/en
Priority to CZ2002832A priority patent/CZ2002832A3/en
Priority to AU2001272368A priority patent/AU2001272368A1/en
Priority to BR0106976-4A priority patent/BR0106976A/en
Priority to IL14852501A priority patent/IL148525A0/en
Priority to PCT/DK2001/000481 priority patent/WO2002004435A1/en
Priority to CA002383963A priority patent/CA2383963A1/en
Priority to SK336-2002A priority patent/SK3362002A3/en
Publication of WO2001002383A8 publication Critical patent/WO2001002383A8/en
Priority to IS6293A priority patent/IS6293A/en
Priority to US10/096,149 priority patent/US20020128497A1/en
Priority to NO20021118A priority patent/NO20021118L/en

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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Transition And Organic Metals Composition Catalysts For Addition Polymerization (AREA)
  • Catalysts (AREA)

Abstract

A new process is described for the synthesis of citalopram characterized by the conversion of 1-(4'-fluorophenyl)1-3-(dimethylaminopropyl)-5-halophthalane in the corresponding Grignard reagent; this intermediate product may be converted into citalopram via intermediate formation of an aldehyde and in the subsequent transformation of the functional group via oxime or hydrazone; or else be converted into citalopram via reaction with compounds containing a cyano group bound to a leaving group. The process described makes it possible to obtain citalopram in high yields, and does not involve the use of drastic conditions of temperature.
PCT/EP2000/006426 1999-07-06 2000-07-06 Process for the synthesis of citalopram WO2001002383A2 (en)

Priority Applications (12)

Application Number Priority Date Filing Date Title
AU64328/00A AU6432800A (en) 1999-07-06 2000-07-06 Process for the synthesis of citalopram
SK336-2002A SK3362002A3 (en) 2000-07-06 2001-07-06 Method for the preparation of citalopram
CA002383963A CA2383963A1 (en) 2000-07-06 2001-07-06 Method for the preparation of citalopram
IL14852501A IL148525A0 (en) 2000-07-06 2001-07-06 Method for the preparation of citalopram
CZ2002832A CZ2002832A3 (en) 2000-07-06 2001-07-06 Process for preparing citalopram
AU2001272368A AU2001272368A1 (en) 2000-07-06 2001-07-06 Method for the preparation of citalopram
BR0106976-4A BR0106976A (en) 2000-07-06 2001-07-06 Method for the preparation of citalopram
EA200200332A EA200200332A1 (en) 2000-07-06 2001-07-06 METHOD OF OBTAINING CYTALOPRAMA
PCT/DK2001/000481 WO2002004435A1 (en) 2000-07-06 2001-07-06 Method for the preparation of citalopram
IS6293A IS6293A (en) 2000-07-06 2002-03-05 Method for producing citalopram
US10/096,149 US20020128497A1 (en) 2000-07-06 2002-03-06 Method for the preparation of citalopram
NO20021118A NO20021118L (en) 2000-07-06 2002-03-06 Process for the preparation of citalopram

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT1999MI001486A ITMI991486A1 (en) 1999-07-06 1999-07-06 PROCESS FOR THE SYNTHESIS OF CITALOPRAM

Publications (3)

Publication Number Publication Date
WO2001002383A2 WO2001002383A2 (en) 2001-01-11
WO2001002383A3 WO2001002383A3 (en) 2001-05-03
WO2001002383A8 true WO2001002383A8 (en) 2001-10-18

Family

ID=11383286

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/006426 WO2001002383A2 (en) 1999-07-06 2000-07-06 Process for the synthesis of citalopram

Country Status (3)

Country Link
AU (1) AU6432800A (en)
IT (1) ITMI991486A1 (en)
WO (1) WO2001002383A2 (en)

Families Citing this family (15)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE237604T1 (en) 1999-04-14 2003-05-15 Lundbeck & Co As H METHOD FOR PRODUCING CITALOPRAM
NL1017417C1 (en) 2000-03-03 2001-03-16 Lundbeck & Co As H Process for the preparation of Citalopram.
GB0005477D0 (en) 2000-03-07 2000-04-26 Resolution Chemicals Limited Process for the preparation of citalopram
AR032455A1 (en) 2000-05-12 2003-11-12 Lundbeck & Co As H METHOD FOR THE PREPARATION OF CITALOPRAM, AN INTERMEDIARY EMPLOYED IN THE METHOD, A METHOD FOR THE PREPARATION OF THE INTERMEDIARY EMPLOYED IN THE METHOD AND PHARMACEUTICAL COMPOSITION ANTIDEPRESSIVE
BR0106976A (en) * 2000-07-06 2002-07-23 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
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
DK1281707T3 (en) * 2001-08-02 2005-05-02 Infosint Sa Process for the preparation of 5-substituted isobenzene furans
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
AR040970A1 (en) 2002-08-12 2005-04-27 Lundbeck & Co As H METHOD FOR THE SEPARATION OF INTERMEDIARIES THAT CAN BE USED FOR THE PREPARATION OF SCITALOPRAM
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
EP2141156A1 (en) 2004-08-23 2010-01-06 Sun Pharma Global FZE Process for Preparation of Citalopram and Enantiomers
CN102503759B (en) * 2011-10-27 2013-10-09 天津大学 Method and device for simultaneously recycling methylbenzene and dimethyl formamide in industrial waste gas by using solvent
CN111533662B (en) * 2020-04-07 2022-08-23 福建海西新药创制有限公司 Synthesis method of citalopram intermediate
CN114763343A (en) * 2021-01-14 2022-07-19 浙江华海药业股份有限公司 Method for purifying citalopram or S-citalopram

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ES2148120T3 (en) * 1997-07-08 2002-01-16 Lundbeck & Co As H METHOD FOR THE PREPARATION OF CITALOPRAM.
ES2149734T3 (en) * 1997-11-11 2003-02-16 Lundbeck & Co As H METHOD FOR THE PREPARATION OF CITALOPRAM.

Also Published As

Publication number Publication date
WO2001002383A3 (en) 2001-05-03
ITMI991486A0 (en) 1999-07-06
AU6432800A (en) 2001-01-22
ITMI991486A1 (en) 2001-01-06
WO2001002383A2 (en) 2001-01-11

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