Method for the preparation of citalopram

Details Method for the preparation of citalopram Method for the preparation of citalopram

C - Chemistry, Metallurgy

07

D

C07D 307/87 (2006.01) A61K 31/34 (2006.01) C07C 215/68 (2006.01) C07C 225/22 (2006.01) C07C 233/33 (2006.01) C07C 233/43 (2006.01) C07D 307/88 (2006.01)

Patent

CA 2291072

A method for the preparation of citalopram is described comprising reaction of a compound of Formula (IV) wherein R1 is H or C1-6alkylcarbonyl successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3- halogen-N,N-dimethylpropylamine, effecting ring closure of the resulting compound of Formula (VI) and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.

L'invention concerne un procédé de préparation de citaloprame consistant à faire réagir un composé de la formule (IV), dans laquelle R?1¿ représente H ou C¿1-6? alkylcarbonyle, successivement, avec un réactif de Grignard de 4-halogèno-fluorophényle et un réactif de Grignard de 3-halogèno-N,N-diméthylpropylamine, à effectuer la cyclisation du composé obtenu de formule (VI), et à transformer le composé 1,3-dihydoisobenzofuranne obtenu en son dérivé 5-cyano correspondant, c'est-à-dire en citaloprame.

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