Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
70523 | Journal of Molecular Catalysis B: Enzymatic | 2010 | 9 Pages |
Abstract
Using two commercial immobilized lipases Lipozyme® TL and Novozym® 435 effective kinetic resolution of several novel 3-aryloxy-1-halogenopropan-2-ols was achieved by acyl transfer reaction in organic solvents, yielding both enantiomers with 89–99% ee. In preparative resolutions carried out in tert-butyl methyl ether at 25 °C with vinyl acetate as acyl donor enantioselectivity ratio E was from 64 to 99. The resolved enantiomers were successfully used as chiral building blocks in the synthesis of new 1-alkylamino-3-aryloxypropan-2-ols, by nucleophilic halogen substitution with isopropylamine and tert-butylamine. The obtained products will be evaluated in vitro as potential new β-adrenergic receptors antagonists.
Related Topics
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Authors
Maciej Maciejewski, Krzysztof Półtorak, Janina E. Kamińska,