Collect. Czech. Chem. Commun. 1986, 51, 1503-1508

Noncataleptic neuroleptic agents: Synthesis of some esters of 2-chloro-10-(4-(2-hydroxyethyl)piperazino)-10,11-dihydrodibenzo[b,f]thiepin

Jiří Jílek, Martin Valchář, Josef Pomykáček, Antonín Dlabač and Miroslav Protiva

Research Institute for Pharmacy and Biochemistry, 130 60 Prague 3


Reactions of 2-chloro-10-(4-(2-hydroxyethyl)piperazino)-10,11-dihydrodibenzo[b,f]thiepin (I) with phenylacetic, methoxyacetic, methylthioacetic, phenoxyacetic and morpholinoacetic acid in dichloromethane and in the presence of N,N'-carbonyldiimidazole gave the title esters II - VI. Reaction of I with succinic anhydride afforded the hemisuccinate VII. The esters prepared elicited ataxia in low doses, were low-cataleptic, but only II, IV, and VII proved some antidopaminergic activity in the test using the affecting dopamine metabolism in rat brain striatum.