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A number of 3‐substituted 6‐piperazinylpyrazolo[3,4‐b]pyridines were synthesized from 2,6‐difluoropyridine by directed ortho metallation and sequential intra‐ and intermolecular displacement of fluorine. Three derivatives with a cyano group in the 3‐position showed activity as selective serotonin re‐uptake inhibitors.

A series of benzisoxazole- and benzisothiazole-3-carboxamides has been prepared and tested for potential antipsychotic activity. In general, the compounds showed an affinity for dopamine D2 and serotonin 5HT2A and 5HT1A receptors. Several members of this series have demonstrated activity in animal models predictive of potential antipsychotic activity. In addition, compounds 18, 19, 22, 27, 28, 43, and 44 have also shown a potential for reduced EPS liability as suggested by the ratio of activity seen in mesolimbic-mediated vs nigrostriatal-mediated behavioral assays.

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