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.
Publication types
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Research Support, Non-U.S. Gov't
MeSH terms
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Adrenergic beta-1 Receptor Antagonists
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Adrenergic beta-2 Receptor Antagonists
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Adrenergic beta-Antagonists / chemical synthesis*
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Adrenergic beta-Antagonists / chemistry
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Crystallography, X-Ray
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Molecular Conformation
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Propanolamines / chemical synthesis*
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Propanolamines / chemistry
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Receptors, Adrenergic, beta-1 / metabolism
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Receptors, Adrenergic, beta-2 / metabolism
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Stereoisomerism
Substances
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Adrenergic beta-1 Receptor Antagonists
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Adrenergic beta-2 Receptor Antagonists
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Adrenergic beta-Antagonists
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Propanolamines
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Receptors, Adrenergic, beta-1
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Receptors, Adrenergic, beta-2
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ICI 118551