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New 4,5-dihydrothieno(2,3 - b ) - benzo(f)thiepines of the general formula and acid addition salts thereof, wherein R represents a hydrogen or halogen atom; R1 represents an alkyl, hydroxyalkyl, acyl or alkoxycarbonyl group with 1 to 4 carbon atoms and n is 2 or 3, are prepared by reacting an ester...

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Hauptverfasser: MIROSLAV RAJSNER, MIROSLAV PROTIVA, JIRINA METYSOVA
Format: Patent
Sprache:dan
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Zusammenfassung:New 4,5-dihydrothieno(2,3 - b ) - benzo(f)thiepines of the general formula and acid addition salts thereof, wherein R represents a hydrogen or halogen atom; R1 represents an alkyl, hydroxyalkyl, acyl or alkoxycarbonyl group with 1 to 4 carbon atoms and n is 2 or 3, are prepared by reacting an ester of an alcohol of the general formula especially a halide, alkyl- or aryl-sulphonate ester thereof, with a secondary amine of the general formula and optionally converting to an acid addition salt. The new 4,5-dihydrothieno (2,3-b )-benzo-(f)thiepines of the first formula above have a polyvalent neurotropic and psychotropic effect and also show central sedative, antihistaminic, antiserotonine and antiemetic effects. 4 - Hydroxy - 4,5 - dihydrothieno - (2,3-b )-benzo(f)thiepine, of the second formula above, is prepared by reacting 2-mercapto-thiophene and o-iodobenzoic acid to give 2-(2-thienylthio) benzoic acid, reducing to the corresponding benzyl alcohol, chlorinating to the corresponding benzyl chloride, forming the corresponding benzyl cyanide, hydrolysing to the corresponding phenylacetic acid, converting to 4,5-dihydrothieno(2,3-b )-benzo(f)thiepine with phosphorus pentoxide and reducing with sodium borohydride.