Multistep solution-phase parallel synthesis of spiperone analogues

Research output: Contribution to journalArticle

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-HT(2A) antagonists with improved selectivity compared to spiperone and AMI-193. (C) 2000 Published by Elsevier Science Ltd.

Details

Authors
  • Henrik C. Hansen
  • Roger Olsson
  • Glenn Croston
  • Carl Magnus Andersson
External organisations
  • ACADIA Pharmaceuticals Inc.
Research areas and keywords

Subject classification (UKÄ) – MANDATORY

  • Pharmaceutical Sciences
Original languageEnglish
Pages (from-to)2435-2439
JournalBioorganic and Medicinal Chemistry Letters
Volume10
Issue number21
Publication statusPublished - 2000 Nov 6
Publication categoryResearch
Peer-reviewedYes
Externally publishedYes