Improvements in or relating to benzothiophene derivatives

摘要

Novel benzothiophene derivatives of the formula (wherein R is C1- 5 alkyl or phenyl which may be C1- 4 alkyl, C1- 4 alkoxy, methylenedioxy, trifluoromethyl, or halogen substituted; R1 is hydrogen, halogen, C1- 5 alkyl or C1- 4 alkoxy; R2 is hydrogen, halogen, C1- 5 alkyl, or C1- 4 alkoxy, or, when R1 is hydrogen, is nitro, amino, hydroxy, C1- 3 acyloxy, C2- 6 dialkylamino or C1- 4 acylamino; A is C1- 4 alkylene; R3 is hydrogen or C1- 5 alkyl; R4 is C1- 5 alkyl or benzyl; or NR3R4 is pyrrolidine, piperidino, hexamethyleneimino, morpholino, dimethyl morpholino, piperazino, methyl or ethyl piperazino, N-benzylpiperazino or tetrahydropyridino) and acid-addition salts thereof are prepared by condensing the appropriate 2-(COR)-3-(OX)-benzothiophene with the appropriate aminoalkyl compound Y-A-NR3R4, wherein X and Y are groups that on condensation form an ether linkage, any amino, imino or hydroxy group being protected and subsequently released by hydrolysis or hydrogenation. Amino and hydroxy products may be acylated and nitro products reduced. Starting materials are prepared by the following processes: The benzothiophenes of the invention, which are stated to have analgesic, antipyretic, antiinflammatory, antitussive, local anaesthetic, antispasmodic and antihistaminic activity, may be made up into pharmaceutical compositions for administration orally, rectally or by injection.