A series of new 5-alkyl and 5-arylisoxazolo [4, 5-d] pyrimidinones (5a–g, 6–8) were prepared from 4-amino-3-oxo-isoxazolidine-5-carboxylic acid amide. Some of the aryl derivatives of isoxazolo [4, 5-d] pyrimidine were tested pharmacologically in comparison with Diazepam. Compounds 5b–d and 7 demonstrated interesting anxiolytic activity.