319427-82-2Relevant academic research and scientific papers
Multistep solution-phase parallel synthesis of spiperone analogues
Hansen, Henrik C.,Olsson, Roger,Croston, Glenn,Andersson, Carl-Magnus
, p. 2435 - 2439 (2007/10/03)
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-HT(2A) antagonists with improved selectivity compared to spiperone and AMI-193. (C) 2000 Published by Elsevier Science Ltd.
