Preparation of citalopram in high yields and purity comprises reacting isobenzofuran compound and cyanide in the presence of palladium catalyst and e.g. copper ions

Preparation of citalopram (I) or its salt comprises reacting a isobenzofuran compound (IV) with (i) a cyanide source in the presence of a palladium catalyst and a catalytic amount of copper I or zinc II ions; or (ii) with zinc cyanide in the presence of a palladium catalyst; and isolating (I). - DET...

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Bibliographic Details
Main Authors SVANE HENRIK, PETERSEN HANS
Format Patent
LanguageEnglish
German
Published 29.06.2001
Edition7
Subjects
APPARATUS THEREFOR
CHEMISTRY
GENERAL METHODS OF ORGANIC CHEMISTRY
HETEROCYCLIC COMPOUNDS
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS
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Summary:Preparation of citalopram (I) or its salt comprises reacting a isobenzofuran compound (IV) with (i) a cyanide source in the presence of a palladium catalyst and a catalytic amount of copper I or zinc II ions; or (ii) with zinc cyanide in the presence of a palladium catalyst; and isolating (I). - DETAILED DESCRIPTION - Preparation of citalopram of formula (I) comprises reacting an isobenzofuran compound of formula (IV) with (i) a cyanide source in the presence of a palladium catalyst and a catalytic amount of copper I or zinc II ions; or (ii) with zinc cyanide in the presence of a palladium catalyst; and isolating (I). - R = halo or CF3(CF2)nSO2; - n = 0-8. - An INDEPENDENT CLAIM is also included for (IV; R = CF3(CF2)nSO2 or iodo).
Bibliography:Application Number: CH20010030820