A chemoenzymatic scalable route to optically active (R)-1-(pyridin-3- yl)-2-aminoethanol, valuable moiety of beta sub(3)-adrenergic receptor agonists

A chemoenzymatic scalable route to optically active (R)-1-(pyridin-3- yl)-2-aminoethanol, valuable moiety of beta sub(3)-adrenergic receptor agonists

Enantiomerically pure (R)-2-chloro-1-(pyridin-3-yl)ethanol has been prepared by kinetic resolution performed in the presence of Candida antarctica SP435-L lipase immobilized on a macroporous polyacrylate resin (Novozym 435 super([registered])). It was converted into (R)-1-(pyridin-3-yl)-2- aminoetha...

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Veröffentlicht in:Bioorganic & medicinal chemistry 2006-02, Vol.14 (4), p.1207-1214
Hauptverfasser: Perrone, Maria Grazia, Santandrea, Ernesto, Giorgio, Erika, Bleve, Laura, Scilimati, Antonio, Tortorella, Paolo
Format: Artikel
Sprache:eng
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Candida antarctica
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Zusammenfassung:Enantiomerically pure (R)-2-chloro-1-(pyridin-3-yl)ethanol has been prepared by kinetic resolution performed in the presence of Candida antarctica SP435-L lipase immobilized on a macroporous polyacrylate resin (Novozym 435 super([registered])). It was converted into (R)-1-(pyridin-3-yl)-2- aminoethanol, left-hand side of beta sub(3)-adrenergic receptor ligands.
ISSN:0968-0896
1464-3391
DOI:10.1016/j.bmc.2005.09.046