Multistep solution-phase parallel synthesis of spiperone analogues
Research output: Contribution to journal › Article
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.
|Research areas and keywords||
Subject classification (UKÄ) – MANDATORY
|Journal||Bioorganic and Medicinal Chemistry Letters|
|Publication status||Published - 2000 Nov 6|