| 摘要 |
Novel compounds of formula <FORM:1098062/C2/1> and pharmaceutically acceptable non-toxic acid addition and quaternary ammonium salts thereof, where A is an alkylene group having not more than 5 carbon atoms and R and R1 are each a hydrogen atom or an alkyl group having not more than 5 carbon atoms, or when taken together they represent tetra-, penta or hexa-methylene, oxatetra-oxapenta- or oxahexa-methylene, azatetra-, azapenta- or azahexa-methylene, or thiatetra-, thiapenta- or thiahexa-methylene, are prepared by reacting a 3-(halogenoalkanoyl) - 5 - phenyl - isoxazole with an amine of formula HNRR1. 3 - Chloroacetyl - 5 - phenylisoxazole used as starting material may be prepared by reacting 3 - chlorocarbonyl - 5 - phenylisoxazole with diazomethane in ether at room temperature and reacting the resultant 3 - diazoacetyl - 5 - phenylisoxazole with dried hydrogen chloride in chloroform at room temperature. Therapeutic compositions, which are useful as antipyretic, analgesic, antitussive and anti-inflammatory agents and which may be adminitered e.g. orally, contain as active ingredients compounds of Formula I above, or pharmaceutically acceptable non-toxic acid-addition and quaternary ammonium salts thereof. |
