Multistep solution-phase parallel synthesis of spiperone analogues

Authors
Hansen, HC Olsson, R Croston, G Andersson, CM
Citation
Hc. Hansen et al., Multistep solution-phase parallel synthesis of spiperone analogues, BIOORG MED, 10(21), 2000, pp. 2435-2439
Citations number
9
Categorie Soggetti
Chemistry & Analysis
Journal title
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
ISSN journal
0960894X → ACNP
Volume
10
Issue
21
Year of publication
2000
Pages
2435 - 2439
Database
ISI
SICI code
0960-894X(20001106)10:21<2435:MSPSOS>2.0.ZU;2-H
Abstract
A flexible, multistep parallel synthesis of spiperone analogues is describe d. A library of 4-substituted piperidines, assembled utilizing reductive am ination and acylation protocols, was alkylated either homogeneously or hete rogeneously, exploiting a product release only concept, to afford an era-se ries of spiperone analogues. Screening of the products at 5-HT2 and D-2 rec eptors revealed 5-HT2A antagonists with improved selectivity compared to sp iperone and AIMI-193. (C) 2000 Published by Elsevier Science Ltd.