Process for preparing sertraline intermediates

Details Process for preparing sertraline intermediates Process for preparing sertraline intermediates

C - Chemistry, Metallurgy

07

C

C07C 249/02 (2006.01) A61K 31/135 (2006.01) C07C 209/26 (2006.01) C07C 209/40 (2006.01) C07C 209/52 (2006.01) C07C 209/88 (2006.01) C07C 211/42 (2006.01) C07C 251/20 (2006.01)

Patent

CA 2448300

A pharmaceutical intermediate, N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)- naphthalenylidene]methanamine, which can be used in the production of sertraline hydrochloride, is conveniently prepared by reacting 4-(3,4- dichlorophenyl)-3,4-dihydro-1-(2H)-naphthalenone with monomethylamine in a solvent which is an amide solvent with a structure of general formula (IV), wherein R1, R3 are indepen dently hydrogen or C1-6 alkyl, which can be substituted, and R2 is hydrogen.

L'invention concerne un intermédiaire pharmaceutique, N-[4-(3,4-dichlorophényl)-3,4-dihydro-1(2H)-naphtalénylidène]méthanamine, pouvant être utilisé dans la production d'hydrochlorure de sertraline, et préparé de manière adéquate par réaction de 4-(3,4-dichlorophényl)-3,4-dihydro-1-(2H)-naphtalénone avec de la monométylamine dans un solvant qui est un solvant amide avec une structure de formule générale (IV). Dans cette formule, R1, R3 représentent indépendamment un atome d'hydrogène ou un alkyle en C¿1?-C¿6?, qui peut être substitué, et R2 représente un atome d'hydrogène.

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