A CHEMOENZYMATIC ROUTE TO BOTH ENANTIOMERS OF BETAXOLOL

Authors
DIBONO G SCILIMATI A
Citation
G. Dibono et A. Scilimati, A CHEMOENZYMATIC ROUTE TO BOTH ENANTIOMERS OF BETAXOLOL, Synthesis, (6), 1995, pp. 699-702
Citations number
21
Categorie Soggetti
Chemistry Inorganic & Nuclear
Journal title
Synthesis → ACNP
ISSN journal
00397881
Issue
6
Year of publication
1995
Pages
699 - 702
Database
ISI
SICI code
0039-7881(1995):6<699:ACRTBE>2.0.ZU;2-1
Abstract
Evaluation of some of the possible lipase-catalyzed transformations ha s been done in order to prepare both enantiomers of betaxolol. Resolut ion of betaxolol by lipase-catalyzed hydrolysis of its bis-acetylated derivatives 4 led to (-)- and (+)-enantiomers with an ee of 20 and 60% , respectively. When the resolution was performed on the chlorohydrin precursor 6 of betaxolol, (-)- and (+)-enantiomers were obtained with an ee of 91 and 75%, respectively.