Issue 22, 2010
From the journal:

Chemical Communications

An efficient asymmetric synthesis of the potent β-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity†‡

James R. Baker,*a   J. Daniel Hothersall,b   Richard J. Fitzmaurice,a   Matthew Tucknott,a   Andy Vinter,a   Andrew Tinkerb  and  Stephen Caddick*a  

* Corresponding authors

a Department of Chemistry, University College London, 20 Gordon St, London, UK
E-mail: j.r.baker@ucl.ac.uk
Fax: +44 (0)2076797463
Tel: +44 (0)2076792653

b Department of Medicine, University College London, 5 University St, London, UK

Abstract

A highly efficient, practical and flexible two-step asymmetric synthesis of the β2-selective β-blocker ICI 118,551 is reported, allowing an unambiguous determination of the dependency of biological activity with optical activity, revealing the S,S-enantiomer to be the most potent.

Graphical abstract: An efficient asymmetric synthesis of the potent β-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity

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Article information

DOI
https://doi.org/10.1039/C0CC00142B
Article type
Communication
Submitted
26 Feb 2010
Accepted
16 Apr 2010
First published
30 Apr 2010

Chem. Commun., 2010,46, 3953-3954

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An efficient asymmetric synthesis of the potent β-blocker ICI-118,551 allows the determination of enantiomer dependency on biological activity

J. R. Baker, J. D. Hothersall, R. J. Fitzmaurice, M. Tucknott, A. Vinter, A. Tinker and S. Caddick, Chem. Commun., 2010, 46, 3953 DOI: 10.1039/C0CC00142B

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