Multistep solution-Phase parallel synthesis of spiperone analogues

…, R Olsson, G Croston, CM Andersson

Index: Hansen, Henrik C.; Olsson, Roger; Croston, Glenn; Andersson, Carl-Magnus Bioorganic and Medicinal Chemistry Letters, 2000 , vol. 10, # 21 p. 2435 - 2439

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Citation Number: 17

Abstract

A flexible, multistep parallel synthesis of spiperone analogues is described. A library of 4- substituted piperidines, assembled utilizing reductive amination and acylation protocols, was alkylated either homogeneously or heterogeneously, exploiting a product release only concept, to afford an oxa-series of spiperone analogues. Screening of the products at 5-HT2 and D2 receptors revealed 5-HT2A antagonists with improved selectivity compared to ...