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Paper | Regular issue | Vol 24, No. 10, 1986, pp.2887-2900
Published online, 1st January, 1970
DOI: 10.3987/R-1986-10-2887
Synthesis and Phermacodynamic Investigation of New Isoguvacine Analogues with Benzoquinolizine Skeleton

Gábor Blaskó, Julianna Kardos, Eszter Baits-Gács, Miklós Simonyi, and Csaba Szántay*

*Central Research Institute for Chemistry, Hungarian Academy of Sciences, H-1025 Budapest, Pusztaszeri ut 59-67, P.O.Box 17, Hungary

Abstract

Stereoisomer hydroxy-esters 15 -19 as well as isoguvacine analogue 20 with benzo[a]quinolizine skeleton have been prepared via regioselective Dieckmann condensation of diester 9 followed by subsequent reduction and E2-elimination. Compounds 16 and 20 have shown a considerable in vitro activity at the GABA/benzodiazepine receptor complex.