C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 307/87 (2006.01)
Patent
CA 2514458
A process for the preparation of citalopram and the pharmaceutically acceptable salts therof is disclosed by reacting 5-cyanophthalide with a 4- fluorophenyl magnesium halide, reducing the 3-hydroxymethyl-4-(4- fluoro~benzoyl)benzonitrile with an agent reducing ketones to alcohols, submitting the thus-obtained 3-hydroxymethyl-4- [(4- fluorophenyl)hydroxymethyl) benzonitrile to a cyclization reaction to give 1- (4-fluorophenyl)-1,3-dihydro-5~isobenzofurancarbonitrile without 1,1-bis(4- fluorophenyl)-1,3-dihydro-5- isobenzofurancarbonitrile and treating 1,1-bis(4 fluorophenyl)-1,3-dihydro-5- isobenzofurancarbonitrile with a 3- (dimetylamino)propyl halide in the presence of a base.
La présente invention concerne un procédé pour préparer du citaloprame et des sels de celui-ci, acceptables du point de vue pharmaceutique, le procédé comprenant les étapes suivantes: réaction d'un 5-cyanophthalide avec un halogénure de 4-fluorophényl magnésium; réduction du 3-hydroxyméthyl-4-(4-fluoro-benzoyl)benzonitrile avec un agent qui réduit les cétones en alcools; exposition du 3-hydroxyméthyl-4-[(4-fluorophényl)hydroxyméthyl]benzonitrile ainsi obtenu à une réaction de cyclisation pour donner du 1-(4-fluorophényl)-1,3-dihydro-5-isobenzofurane carbonitrile sans 1,1-bis(4-fluorophényl)-1,3-dihydro-5- isobenzofurane carbonitrile; et traitement du 1,1-bis(4-fluorophényl)-1,3-dihydro-5- isobenzofurane carbonitrile avec un halogénure de 3-(dimétylamino)propyle en la présence d'une base.
Cotticelli Giovanni
Dall'asta Leone
Di Lernia Gianluca
Adorkem Technology Spa
Riches Mckenzie & Herbert Llp
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