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Multistep solution-phase parallel synthesis of spiperone analogues

Hansen, Henrik C. LU ; Olsson, Roger LU ; Croston, Glenn and Andersson, Carl Magnus (2000) In Bioorganic and Medicinal Chemistry Letters 10(21). p.2435-2439
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.

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author
; ; and
publishing date
type
Contribution to journal
publication status
published
subject
in
Bioorganic and Medicinal Chemistry Letters
volume
10
issue
21
pages
2435 - 2439
publisher
Elsevier
external identifiers
  • pmid:11078195
  • scopus:0034613562
ISSN
0960-894X
DOI
10.1016/S0960-894X(00)00483-2
language
English
LU publication?
no
id
5c9a51b1-5686-469b-ba82-a31753916d93
date added to LUP
2019-10-02 10:39:37
date last changed
2020-09-01 12:45:08
@article{5c9a51b1-5686-469b-ba82-a31753916d93,
  abstract     = {<p>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-HT<sub>2</sub> and D<sub>2</sub> receptors revealed 5-HT(2A) antagonists with improved selectivity compared to spiperone and AMI-193. (C) 2000 Published by Elsevier Science Ltd.</p>},
  author       = {Hansen, Henrik C. and Olsson, Roger and Croston, Glenn and Andersson, Carl Magnus},
  issn         = {0960-894X},
  language     = {eng},
  month        = {11},
  number       = {21},
  pages        = {2435--2439},
  publisher    = {Elsevier},
  series       = {Bioorganic and Medicinal Chemistry Letters},
  title        = {Multistep solution-phase parallel synthesis of spiperone analogues},
  url          = {http://dx.doi.org/10.1016/S0960-894X(00)00483-2},
  doi          = {10.1016/S0960-894X(00)00483-2},
  volume       = {10},
  year         = {2000},
}