Method for preparing sertraline
AssigneeOrion Corporation Fermion
InventorIlpo Laitinen
Life of this patent
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Abstract
(1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine (sertraline) may be prepared by hydrogenating of N-[4-(3,4-dichlorophenyl)-3, 4-dihydro-1(2H)-naphthalenylidene]methanamine in the presence of a dehalogenation inhibitor, e.g., triphenylphosphite or trimethylphosphite and a catalyst.
Claims17
A process for the preparation of cis-sertraline, comprising hydrogenating N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine in the presence of a catalyst and a dehalogenation inhibitor, to obtain cis-racemate of 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine.
A process for the preparation of (1S-cis)-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine or an acid addition salt thereof, comprising:
- hydrogenating N-[4-(3,4-dichlorophenyl)-3,4-dihydro-1(2H)-naphthalenylidene]methanamine in the presence of a catalyst and a dehalogenation inhibitor, to obtain cis-racemate of 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine;
- and
- resolving said cis-racemate of 4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamine, to obtain the (+)enantiomer of cis-4-(3,4-dichlorophenyl)-1,2,3,4-tetrahydro-N-methyl-1-naphthalenamime.
Dependencies are inferred from the claim text.