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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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Publication details

The article was received on 26 Feb 2010, accepted on 16 Apr 2010 and first published on 30 Apr 2010


Article type: Communication
DOI: 10.1039/C0CC00142B
Citation: 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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