D'AMICO M

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The synthesis in excellent yields of 2,3-dihydro-6-mercapto-1,3,5-triphenyl-2-thioxo-4(3H)-pyrimidinone 3 and 5-ethoxycarbonyl-2,3-dihydro-6-mercapto-1,3-diphenyl-2-thioxo-4(3H)-pyrimidinone 4 by reaction of Me phenylacetate or di-Et malonate, resp., with Ph isothiocyanate (3 molar equivalents) and sodium hydride (2 molar equivalents) in DMF...

The synthesis of 4-amino-3,5-diphenyl-1H-pyrazole-1-ethanol, as well as of its N-Me, N-Et and N,N-di-Me derivs. is described. A series of 1-(2-alkylaminoethyl)-3,5-diphenyl-1H-pyrazole-4-amines and of N-substituted 4-dimethylamino-3,5-diphenyl-1H-pyrazole-1-ethanamines were also prepd. Some of the above compds. showed marked local anesthetic...

The synthesis of 5-[[ω-(dialkylamino)alkoxy]methylene]-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-ones (I, n = 2, 3; NR2 = NEt2, 1-hexahydroazepinyl, etc.) by reaction of (+)-5-(hydroxymethylene)-1,3,3-trimethyl-2-oxabicyclo[2.2.2]octan-6-one with a series of ω-(chloroalkyl)dialkylamines in the presence of potassium carbonate is described. ...

The synthesis of (+)-1,7,7-trimethylbicyclo[2.2.1]heptan-2-one O-[ω-(dialkylamino)alkyl]oximes by reaction of (+)-camphoroxime sodium salt with a series of ω(chloroalkyl)dialkylamines in DMF soln. is described. Some of the above compds. showed strong hypotensive, antiinflammatory, analgesic and local anesthetic activity in rats and mice, as...