| 摘要 |
<p>(I) (in which R is H) and its N-substitution products (II): (where R is opt. substd. 1-7C alkyl, aralkyl, 3-5C alkenyl or acyl) and their non-toxic acid addn. or quaternisation products with acids or alkyl halides, are active ingredients in analgesic or antipyretic compns. (I) is pref. prepd. by (a) brominating 3r-N,N-dimethylamino-4c-phenyl-4t-ethoxycarbonyl-cyclohexene-(1) (III) in a chlorohydrocarbon, particularly CHCl3, at -15 to 0 degrees C (-10 degrees C) and treating product with water; or (b) (in lesser yield) by heating (III) with Hg(II) acetate in aqs. acetic acid at elevated, partic. boiling temp. of 10% acetic acid; or (c) reacting (III) with gaseous O2 in presence of precious metal catalyst, such as PtO2, in an inert solvent, such as benzene, and if necessary converting (I) to (II) by reacting with (amino)alkyl halides, acyl halides and isocyanates.</p> |
