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.
Please use this url to cite or link to this publication:
https://lup.lub.lu.se/record/5c9a51b1-5686-469b-ba82-a31753916d93
- author
- Hansen, Henrik C.
LU
; Olsson, Roger
LU
; Croston, Glenn
and Andersson, Carl Magnus
- publishing date
- 2000-11-06
- 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
-
- scopus:0034613562
- pmid:11078195
- 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
- 2024-01-01 21:29:31
@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}},
}