WO2002048133A3 - A process for the preparation of citalopram - Google Patents

A process for the preparation of citalopram Download PDF

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Publication number
WO2002048133A3
WO2002048133A3 PCT/EP2001/014523 EP0114523W WO0248133A3 WO 2002048133 A3 WO2002048133 A3 WO 2002048133A3 EP 0114523 W EP0114523 W EP 0114523W WO 0248133 A3 WO0248133 A3 WO 0248133A3
Authority
WO
WIPO (PCT)
Prior art keywords
compound
citalopram
formula
preparation
halo
Prior art date
Application number
PCT/EP2001/014523
Other languages
French (fr)
Other versions
WO2002048133A2 (en
Inventor
Giuseppe Guazzi
Original Assignee
C D Farmasint S R L
Giuseppe Guazzi
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 C D Farmasint S R L, Giuseppe Guazzi filed Critical C D Farmasint S R L
Priority to AU2002229648A priority Critical patent/AU2002229648A1/en
Publication of WO2002048133A2 publication Critical patent/WO2002048133A2/en
Publication of WO2002048133A3 publication Critical patent/WO2002048133A3/en

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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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Steroid Compounds (AREA)

Abstract

A process for the preparation of Citalopram comprising the transformation of a compound of formula (VII), wherein R is C1-C4 alkyl. Compound (VII) is reacted in sequence with a Grignard reagent of a 4-halo fluorobenzene and a Grignard reagent of a 3-halo-N,N-dimethylpropylamine, respectively, giving a compound of formula (V), wherein R is as defined above. (V) Is hydrolysed to a compound of formula (IV), which is converted to a 5-oxime (III) by means of hydroxylamine, submitted to cyclization and converted to the corresponding 5-cyano derivative, i.e. Citalopram.
PCT/EP2001/014523 2000-12-12 2001-12-11 A process for the preparation of citalopram WO2002048133A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU2002229648A AU2002229648A1 (en) 2000-12-12 2001-12-11 A process for the preparation of citalopram

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
ITMI2000A002674 2000-12-12
ITMI20002674 IT1319686B1 (en) 2000-12-12 2000-12-12 CITALOPRAM PREPARATION PROCEDURE.

Publications (2)

Publication Number Publication Date
WO2002048133A2 WO2002048133A2 (en) 2002-06-20
WO2002048133A3 true WO2002048133A3 (en) 2002-11-14

Family

ID=11446211

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2001/014523 WO2002048133A2 (en) 2000-12-12 2001-12-11 A process for the preparation of citalopram

Country Status (3)

Country Link
AU (1) AU2002229648A1 (en)
IT (1) IT1319686B1 (en)
WO (1) WO2002048133A2 (en)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8440822B2 (en) 2007-04-18 2013-05-14 Michael Joseph Luzzio Sulfonyl amide derivatives for the treatment of abnormal cell growth

Families Citing this family (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1281708B1 (en) * 2001-08-02 2004-05-26 Infosint Sa Process for the preparation of 5-Formylphthalide
DK1281707T3 (en) * 2001-08-02 2005-05-02 Infosint Sa Process for the preparation of 5-substituted isobenzene furans
IS7239A (en) * 2001-12-14 2004-04-29 H. Lundbeck A/S Process for the production of acitalopram
FI20021421A0 (en) * 2002-07-30 2002-07-30 Orion Corp Fermion Production Process
AU2002330730A1 (en) * 2002-08-14 2004-03-03 Natco Pharma Limited Process for the preparation of high purity citalopram and its pharmaceutically acceptable salts
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

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4136193A (en) * 1976-01-14 1979-01-23 Kefalas A/S Anti-depressive substituted 1-dimethylaminopropyl-1-phenyl phthalans
WO1998019512A2 (en) * 1997-11-11 1998-05-14 H. Lundbeck A/S Method for the preparation of citalopram
WO1998019513A2 (en) * 1997-07-08 1998-05-14 H. Lundbeck A/S Method for the preparation of citalopram
WO1998019511A2 (en) * 1997-11-10 1998-05-14 H. Lundbeck A/S Method for the preparation of citalopram
WO1999030548A2 (en) * 1999-04-14 1999-06-24 H. Lundbeck A/S Method for the preparation of citalopram

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4136193A (en) * 1976-01-14 1979-01-23 Kefalas A/S Anti-depressive substituted 1-dimethylaminopropyl-1-phenyl phthalans
WO1998019513A2 (en) * 1997-07-08 1998-05-14 H. Lundbeck A/S Method for the preparation of citalopram
WO1998019511A2 (en) * 1997-11-10 1998-05-14 H. Lundbeck A/S Method for the preparation of citalopram
WO1998019512A2 (en) * 1997-11-11 1998-05-14 H. Lundbeck A/S Method for the preparation of citalopram
WO1999030548A2 (en) * 1999-04-14 1999-06-24 H. Lundbeck A/S Method for the preparation of citalopram

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
PERKIN W H ET AL: "AN INCESTIGATION OF THE ACTION OF HALOGENS ON 2:4-DIMETHYLBENZOYL CHLORIDE", JOURNAL OF THE CHEMICAL SOCIETY, CHEMICAL SOCIETY, LONDON, GB, no. 127, 1925, pages 2275 - 2297, XP001063238, ISSN: 0368-1769 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US8440822B2 (en) 2007-04-18 2013-05-14 Michael Joseph Luzzio Sulfonyl amide derivatives for the treatment of abnormal cell growth

Also Published As

Publication number Publication date
IT1319686B1 (en) 2003-10-23
ITMI20002674A1 (en) 2002-06-12
WO2002048133A2 (en) 2002-06-20
AU2002229648A1 (en) 2002-06-24

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