A chemoenzymatic scalable route to optically active (R)-1-(pyridin-3-yl)-2-aminoethanol, valuable moiety of beta3-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). It was converted into (R)-1-(pyridin-3-yl)-2-aminoethanol, left-hand side of beta(3)-adrenergic receptor ligands.
Perrone
Maria Grazia
MG
Dipartimento Farmaco-Chimico, Università degli Studi di Bari, Italy.
Santandrea
Ernesto
E
Giorgio
Erika
E
Bleve
Laura
L
Scilimati
Antonio
A
Tortorella
Paolo
P
D058667:Adrenergic beta-3 Receptor Agonists; D002175:Candida / Q000201:enzymology; D004800:Enzymes, Immobilized / Q000378:metabolism; D004983:Ethanolamines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D007700:Kinetics; D008049:Lipase / Q000378:metabolism*; D008958:Models, Molecular; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D022702:Receptors, Adrenergic, beta-3 / Q000378:metabolism; D013237:Stereoisomerism
C508669:(R)-1-(pyridin-3-yl)-2-aminoethanol; D058667:Adrenergic beta-3 Receptor Agonists; D004800:Enzymes, Immobilized; D004983:Ethanolamines; D011725:Pyridines; D022702:Receptors, Adrenergic, beta-3; D008049:Lipase