process for the preparation of medicines with a force on the central nervous system and cardiovascular function.formed drug del with such force and method for the preparation of medicinal compounds.

摘要

1458537 Butanoic and butenoic acid derivatives ASPRO-NICHOLAS Ltd 3 Dec 1974 [15 Dec 1973] 58202/73 Heading C2C Novel "alkyl" (including unsaturated hydrocarbon radicals) esters, di-"alkyl"-amides and saturated heterocyclic amides of 4-amino- "alkyl" - 4 - phenyl - 4 - cyano - butanoic and but-2-enoic acids which are substituted in at least one of the two and three positions by an "alkyl" group of 1-4 C or by a divalent "alkylene" (including unsaturated hydrocarbon radicals) radical which together with at least one of the carbon atoms at said two and three positions forms a stable carbocyclic ring of 3-8 C and which are optionally substituted, except in the said "alkyl" or "alkylene" groups in the two and/or three positions, by therapeutically compatible substituents and acid addition salts thereof are prepared by reaction of a corresponding 4 - aminoalkyl - 4 - cyano - 4 - phenyl -1- alkoxy or alkylthio-1-dialkylamino or saturated heterocyclic amino-but-1-ene or buta-1,2-diene with a strong non-nucleophilic acid in the presence of a primary alcohol and an orthoester and hydrolysing the resultant product; reaction of an alkali metal alpha-aminoalkylbenzyl cyanide with an alkyl ester of a corresponding prop-1-enoic acid having a suitable leaving group in the 3-position; reaction of an alkali metal alpha-aminoalkylbenzyl cyanide with a dialkyl ester of a corresponding ethylene-1,1- dicarboxylic acid or reaction of a corresponding 4 - amino - alkyl - 4 - cyano - 4 - phenyl - 1- alkoxy or alkylthio-1-dialkylamino or heterocyclic amino-but-1-ene or buta-1,2-diene with NaI and a strong acid. Pharmaceutical compositions in the form of tablets, capsules, suppositories, solutions and suspensions comprise one of the above novel compounds together with a suitable carrier and are useful as CNS- or cardiovascular-active agents.