GB866432A - New carboxylic acid amides substituted at the nitrogen atom and ª--carbon atom - Google Patents

Abstract

The invention comprises amides of the general formula: <FORM:0866432/IV (b)/1> (wherein R represents hydrogen or a methyl or ethyl group, R1 represents hydrogen or a C1-4 alkanoyl radical, R2 represents a C1-4 alky radical, and R3 represents hydrogen or a C1-4 alkyl or alkoxy radical), medicinal preparations containing them (see Group VI), and the preparation of the amides by the following processes: (a) reacting the appropriate aralkylamine with the appropriate acid or functional derivative thereof (preferably one in which R1 represents an alkanoyloxy radical, which, if a final product in which R1 represents hydrogen is required, should be capable of subsequently being easily split off, e.g. by alkaline or acid hydrolysis); (b) (when R1=H) reducing the corresponding b -ketocarboxylic acid amides; (c) (when R1=H) treating the corresponding b -aminocarboxylic acid amines with an alkali metal nitrite in the presence of a dilute mineral acid; and (d) (when R1= alkanoyl) acylating the compounds in which R1=H). b -Keto-valeric and -caproic acid aralkylamides are prepared by reacting the corresponding acetoacetic acid aralkylamides (prepared from diketene and the appropriate arakylamines) with a propionyl or butyryl halide and then eliminating the a -acetyl group by acid or alkaline hydrolysis. b - Aminobutyric acid-[2-ethyl-2-phenyl-n-butyl-(1)]-amide is prepared by catalytic hydrogenation of acetoacetic a acid-[2-ethyl-2-phenyl-n-butyl-(1)]-amide in methanol saturated with ammonia. Specification 645,886 is referred to.ALSO:A medicinal preparation comprises an amide of the formula <FORM:0866432/VI/1> (wherein R is hydrogen, methyl or ethyl, R1 is hydrogen or a C1-4 alkanoyl radical, R2 is a C1-4 alkyl radical and R3 is hydrogen or a C1-4 alkyl or alkoxy radical) and a pharmaceutically suitable carrier. Tablets and injection solutions are referred to. Specification 648,886 is referred to.