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

  • Chem Commun (Camb). 2010 Jun 14;46(22):3953-4. doi: 10.1039/c0cc00142b.
James R Baker  1 ,  J Daniel Hothersall ,  Richard J Fitzmaurice ,  Matthew Tucknott ,  Andy Vinter ,  Andrew Tinker ,  Stephen Caddick
Affiliations
  • 1. Department of Chemistry, University College London, 20 Gordon St, London, UK. [email protected]
PMID: 20431838 DOI: 10.1039/c0cc00142b
Abstract

A highly efficient, practical and flexible two-step asymmetric synthesis of the beta(2)-selective beta-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.

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