Abstract
A simple and efficient synthesis of novel 6-aminomethyl-tetrahydroindol-4-ones, which are butyrophenone analogues of molindone, is described. These compounds exhibit potent affinities for D 2 and 5-HT 2A receptors in vitro. The most active compounds, 6d (QF 0408B) and 6e (QF 0409B), with pK i (5-HT 2A/D 2) ratios of 1.32 and 1.17 respectively, show an antipsychotic profile according to Meltzer's classification.
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