Collect. Czech. Chem. Commun. 1987, 52, 1073-1078

4-Amino-1-(4-cyclopentylphenyl)butan-1-ones; Synthesis and biological screening

Zdeněk Vejdělek and Miroslav Protiva

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


4-Chloro-1-(4-cyclopentylphenyl)butan-1-one (IX), obtained by Friedel-Crafts reaction of cyclopentylbenzene with 4-chlorobutanoyl chloride, was subjected to substitution reactions with 4-phenylpiperidin-4-ol and a series of N-monosubstituted piperazines, and gave the title compounds I-VIII. Their salts underwent biological screening in various lines. Only compounds I, V, and VII showed clear indications of tranquillizing activity (ataxia, thiopental potentiation, hypothermic effect, inhibition of locomotor activity, antiamphetamine effect).