Process for the preparation of tetralone imines for the...

Details Process for the preparation of tetralone imines for the... Process for the preparation of tetralone imines for the...

C - Chemistry, Metallurgy

07

D

C07D 249/02 (2006.01) C07C 249/02 (2006.01) C07C 251/20 (2006.01)

Patent

CA 2328778

4-(3,4-Dichlorophenyl)-3,4-dihydro-2H-naphthalen-1-ylidene-methylamine and related analogs are prepared form .alpha.-tetralone by a facile three-step process. This compound is the required intermediate to prepare sertraline, (1S- cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetra-hydro-N-methyl-1-naphthylamine. Sertraline has selective serotonin uptake inhibitor activity making it a valuable antidepressant pharmaceutical product.

Selon l'invention, on prépare une 4-(3,4-dichlorophényl)-3,4-dihydro-2H-naphtalèn-1-ylidène-méthylamine et des analogues de celle-ci, à partir d'alpha-tétralone, à l'aide d'un procédé facile en trois étapes. Ce composé constitue l'intermédiaire nécessaire à la préparation de sertraline, (1S-cis)-4-(3,4-dichlorophényl)-1,2,3,4-tétra-hydro-N-méthyl-1-naphtylamine. La sertraline possède une activité inhibitrice de l'accumulation de la sérotonine, ce qui en fait un produit pharmaceutique antidépresseur précieux.

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