4-/4'-halophenyl/-2-methyl-1,2,3,4-tetrahydroisoquinolines...

C - Chemistry – Metallurgy – 07 – D

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C07D 217/14 (2006.01)

Patent

CA 2015114

ABSTRACT OF THE DISCLOSURE: 4-/4'-halophenyl/2-methyl-1,2,3,4-tetrahydroiso- quinoline racemate or optically active isomer having the formula: Image wherein R is a member selected from brome or fluor, and their physiologically acceptable salts. These have high inhibitory effect towards dopamine noradrenaline or serotonin uptake, as well as high antiulcer activity. A method for the preparation, is characterised in that benzylmethylamine is alkylated with at least one .alpha.- halogenated aryl aliphatic ketone to 2-/N-methyl-N- benzylamin/-4-haloacetophenone, and then reduced to N- benzyl-2-methylamine-1-/4-halophenyl/-1-ethanol with sodium borhydrate. The latter is cyclodehydrated with concentrated sulphuric acid.

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