1-(3-Hydroxyphenyl)-2-[3-phenyl-2-methylpropyl-(2)-amino]-aethynol-(1)

摘要

1-(3-Hydroxyphenyl)-2-(3-phenyl-2-methylprop-2-ylamino)-ethan-1-o- l Analgesic and anti-inflammatory agent. Oral LD50 in mice 725 mg/kg.; i.v. LD50 in mice 34 mg/kg. Single oral doses of 10-300 mg/kg. against kaolin- and carrageenin-induced oedema in the rat have a similar effect to that of 2,3-dimethyl-4-dimethylamino-1-phenyl-3-pyrazolin-5-one. An oral dose of 100 mg/kg reduces oedema by 30%. Single doses of 25-50 mg/kg. of the cpd. in rabbits increases the pain threshold by 30-60% when their dental pulp is electrically stimulated. 2-(3-Phenyl-2-methylpropylamino)-3'-hydroxy-acetophenone (65.4 g.) in methanol (400 ml) was hydrogenated over PtO2 (1.2 g.) at 45 deg.C and 2 atmos. in a rocking hydrogenator for 2 hrs. The catalyst was filtered off, washed with methanol and the combined filtrates were evap. The residue was dissolved in ether, the soln. was washed with water, dried and the solvent distilled. The residue was crystallised by cooling and seeding to give the title compound.