| 摘要 |
1416705 Keto-esters DUNCAN FLOCKHART & CO Ltd 26 June 1973 [14 July 1972] 33070/72 Heading C2C The invention comprises novel compounds (I) or pharmaceutically acceptable acid addition salts thereof, wherein X is an oxygen or sulphur atom, R 1 is (1) a straight or branched chain alkyl group, (2) a cycloalkyl group, (3) an alkenyl group, (4) an alkynyl group, (5) an aralkyl group, (6) an aryl group, (7) a pyridyl group, (8) a group of the formula (9) a group of the formula in which Y is a perhalogenoalkyl, hydroxy, hydroxyalkoxy, hydroxyalkoxyalkoxy, alkoxy, alkoxyalkoxy, acyloxy or alkoxycarbonyl group or Y is a -S-(CH 2 ) n OZ group, in which Z is an acyl group, m and n which may be the same or different, each represent integers of 1 to 3. R 2 is (1) a hydrogen atom, (2) a straight or branched chain alkyl group, optionally substituted by one or more alkoxy or alkoxycarbonyl groups, (3) an alkoxycarbonyl group, (4) a cycloalkyl group, (5) a cycloalkenyl group, (6) an aryl, aralkyl or aralkenyl group in which the aryl portion may optionally be substituted by one or more alkyl, alkoxy, alkoxyalkyl, methylenedioxy, alkoxycarbonyl, perhalogenoalkyl, nitro, halogen, nitrile, aryl, dialkylaminocarbonyl, amino, alkylamino, dialkylamino or aralkoxy groups, (7) a saturated or unsaturated heterocyclic ring containing one or more heteroatoms and which ring may be optionally substituted by alkyl, (8) a group of the formula or (9) a group of the formula R 3 is (1) a hydrogen atom, (2) a straight or branched chain alkyl group, which may be substituted with alkoxycarbonyl, carboxyl, amino, alkylamino, dialkylamino, or heterocyclic groups, (3) an alkenyl group which may be substituted with an alkyl carbonyl or alkoxycarbonyl group, (4) an alkynyl group, or (5) an aralkyl group. R 4 is either (1) a straight or branched chain alkyl group, (2) an alkoxyalkyl group, (3) an alkenyl group, or (4) an aralkyl group, R 5 is a hydrogen atom, an alkyl, aryl or alkoxycarbonyl group, and R 6 is a hydrogen atom, or an alkyl or aryl group; with the proviso that when R 1 and R 4 are ethyl groups, and R 3 , R 5 and R 6 are hydrogen atoms then R 2 may not be a methyl group. They are made by standard methods using compounds (IIb) and (IV) (IIb can exist in various tautomeric forms). Pharmaceutical preparations having a CNS depressant effect and anaesthetic and analgesic actions contain (I) as active ingredient; administration is orally or parenterally.
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