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|Abstract:||(R)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, its preparation and pharmaceutical compositions containing the same. It can be prepared either by reacting (R)-alpha-ethyl-2-oxo-1-pyrrolidineactic acid successively with an alkyl haloformate and with ammonia, or, by cyclizing an (R)-2-amino-butanamide of the formula X--CH.sub.2 CH.sub.2 --Y--NHCH (C.sub.2 H.sub.5)CONH.sub.2 wherein Y is a --CH.sub.2 --radical when X represents a ZOOC--radical and Y is a --CO--radical when X represents a HalCH.sub.2 --radical, Z being a C.sub.1 -C.sub.4 alkyl radical and Hal a halogen atom. This dextrorotatory enantiomer has been found to have significantly higher mnemic activity and lower toxicity than the corresponding racemate.|
|Inventor(s):||Gobert; Jean (Brussels, BE), Giurgea; Corneliu (Brussels, BE), Geerts; Jean-Pierre (Leglise, BE), Bodson; Guy (Bellefontaine, BE)|
|Assignee:||UCB Societe Anonyme (Brussels, BE)|
|Filing Date:||Mar 12, 1987|
|Claims:||1. A pharmaceutical composition comprising a therapeutically effective amount of (R)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide and a pharmaceutically acceptable solid or liquid diluent or carrier therefor, said composition being substantially free of (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide. |
2. (R)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide substantially free of (S)-alpha-ethyl-2-oxo-1-pyrrolidineacetamide, prepared by a process which comprises cyclizing, in an inert solvent and in the presence of a basic substance, an (R)-2-amino-butanamide of the formula
X represents ZOOC-- or HalCH.sub.2 -- wherein Z is alkyl of 1 to 4 carbon atoms and Hal a halogen atom, and
Y represents --CH.sub.2 -- or --CO--,
with the proviso that Y is --CH.sub.2 -- when X represents ZOOC--, and Y is --CO-- when X represents HalCH.sub.2 --.
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