| 摘要 |
<p>1329590 Amino-oxy carboxylic acid amides RICHTER GEDEON VEGYESZETI GYAR RT 23 Dec 1970 [29 Dec 1969] 61177/70 Heading C2C [Also in Division A5] The invention comprises amino-oxy carboxylic acid amides of the Formula I wherein X is H or a carboxylic acyl group, R is H or an unsubstituted or substituted alkyl, aralkyl or aryl, and Z is an unsubstituted or substituted C 1-15 alkyl, cycloalkyl, aryl, aralkyl or heterocyclic radical, provided that X is not benzoyl when R is H, the pharmaceutically acceptable acid addition salts of those compounds capable of forming them, and/or the optically active isomers of such compounds containing asymmetric carbon atoms and their preparation and the preparation of compounds of the above Formula I in which X is benzoyl and R is H. The compounds are prepared by reacting compounds of the Formula II or reactive derivatives thereof, wherein A is a carboxylic acyl group, or when in the end product X is H, A is a radical capable of temporarily protecting the amino group, with amines of the formula and, if present, removing the protecting group from the resulting amides of the formula and, if desired, acylating the compounds of Formula I thus obtained in which X is H. N - (Benzyloxycarbonylglycyl)amino-oxyacetanilide is obtained by reacting amino-oxyacetanilide hydrochloride with benzyloxycarbonylglycine pentachlorophenyl ester. 2 - Benzyloxycarbonylamino-oxyacetyl chloride is made by treating the corresponding free acid with phosphorus pentachloride. 2 - Amino-oxy - 6 - benzyloxycarbonylaminohexanilide is prepared by reacting aniline with 2 - amino-oxy-6-benzyloxycarbonylhexanoic acid resulting from the hydrolysis of the corresponding dicyclohexylammonium salt.</p> |
