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filingDate 1974-09-03-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationDate 1977-01-19-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber GB-1461667-A
titleOfInvention Amphetamine derivatives
abstract 1461667 Amphetamine derivatives ASTRA LAKEMEDEL AB 3 Sept 1974 [4 Sept 1973] 38499/74 Heading C2C Novel compounds of Formula I wherein each of R<SP>1</SP> and R<SP>2</SP>, which may be the same or different, is a hydrogen or halogen atom, or a lower alkyl group, R<SP>3</SP> is a lower alkyl group or a benzyl group, R<SP>4</SP> is a hydrogen atom, a lower alkyl group, a benzyl group or a -CH 2 CH 2 CH 2 -bridge attached to the phenyl ring at the ortho-position relative to the N- substituent on the phenyl ring, R<SP>5</SP> is a hydrogen atom or a methyl group and R<SP>6</SP> is a lower alkyl group, with the proviso that when each of R<SP>3</SP> and R<SP>4</SP> is a methyl group and R<SP>5</SP> is a hydrogen atom, R<SP>1</SP> and/or R<SP>2</SP> is a lower alkyl group or a halogen atom; or a pharmaceutically acceptable acid addition salt thereof where "lower" denote groups containing up to 5 carbon atoms, are prepared by one of the following methods (a) a compound of Formula II is reduced; (b) a compound of Formula II wherein R<SP>3</SP> is benzoyl or C 1-5 acyl is reduced; (c) introduction of R 1 or R 2 = halogen by direct halogenation of a compound of Formula I above wherein R 1 and/or R 2 are H; or (d) hydrolysis of a compound of Formula IV wherein Z is a C 1-5 acyl group. Intermediates of Formula II above are prepared by reaction of R<SP>6</SP>CH 2 NO 2 and ammonium acetate with a compound of Formula III which itself is obtained by formylation of a compound of Formula VI by the Vilsmeyer-Haack reaction with OMF and POCl 3 . Compounds of Formula VI above are obtained by alkylation of the primary amine. Intermediates of Formula IV above are obtained by the reaction Pharmaceutical compositions in conventional forms for oral, rectal orparenteral administration and having antidepressant and anxiolytic activity comprise an above novel compound and a carrier therefor.
priorityDate 1973-09-04-04:00^^<http://www.w3.org/2001/XMLSchema#date>
type http://data.epo.org/linked-data/def/patent/Publication

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Total number of triples: 42.