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Synthesis 1995; 1995(6): 699-702
DOI: 10.1055/s-1995-3965
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A Chemoenzymatic Route to Both Enantiomers of Betaxolol

Giuseppe Di Bono, Antonio Scilimati*
  • *Dipartimento Farmaco-Chimico, Università di Bari, Via Orabona n. 4, I-70125 Bari, Italy
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Publication History

Publication Date:
31 December 2000 (online)

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Evaluation of some of the possible lipase-catalyzed transformations has been done in order to prepare both enantiomers of betaxolol. Resolution of betaxolol by lipase-catalyzed hydrolysis of its bisacetylated 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.

betaxolol - kinetic resolution - lipase

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