C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 307/87 (2006.01) A61K 31/343 (2006.01) A61P 25/24 (2006.01) C07C 69/76 (2006.01) C07C 229/38 (2006.01) C07C 235/84 (2006.01) C07C 237/30 (2006.01)
Patent
CA 2291067
A method for the preparation of citalopram comprising the steps of reacting a compound of Formula (IV) wherein R1 is C1-6 alkyl and X is O or NH, successively with a Grignard reagent of 4-halogen-fluorophenyl and a Grignard reagent of 3-halogen-N,N-dimethyl-propylamine, respectively, effecting ringclosure of the resulting compound of Formula (V) wherein R1 and X are as defined above, and converting the resulting 1,3-dihydroisobenzofuran compound to the corresponding 5-cyano derivative, i.e. citalopram.
Procédé de préparation de citalopram consistant à faire réagir un composé de formule (IV), dans laquelle R?1¿ représente alkyle C¿1-6? et X représente O ou NH, successivement avec un réactif grignard, de 4-halogène-fluorophényle et un réactif grignard, de 3-halogène-N,N-diméthyl-propylamine, respectivement, à fermer le cycle du composé résultant de la formule (V), dans laquelle R?1¿ et X sont définis ci-avant, et à convertir le composé 1,3-dihydroisobenzofuran en dérivé 5-cyano correspondant, c'est-à-dire en citalopram.
Goudreau Gage Dubuc
H. Lundbeck A/s
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