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Issue 22, 2010
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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

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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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Supplementary files

Article information


Submitted
26 Feb 2010
Accepted
16 Apr 2010
First published
30 Apr 2010

Chem. Commun., 2010,46, 3953-3954
Article type
Communication

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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