Biocatalysis offers an alternative approach to conventional chemical processes for the production of single-isomer chiral drugs. Lipases are one of the most used enzymes in the synthesis of enantiomerically pure intermediates. The use of this type of enzyme is mainly due to the characteristics of their regio-, chemo- and enantioselectivity in the resolution process of racemates, without the use of cofactors. Moreover, this class of enzymes has generally excellent stability in the presence of organic solvents, facilitating the solubility of the organic substrate to be modified. Further improvements and new applications have been achieved in the syntheses of biologically active compounds catalyzed by lipases. This review critically reports and discusses examples from recent literature (2007 to mid-2015), concerning the synthesis of enantiomerically pure active pharmaceutical ingredients (APIs) and their intermediates in which the key step involves the action of a lipase.

Carvalho, A., Fonseca, T., De Mattos, M., De Oliveira, M., De Lemos, T., Molinari, F., et al. (2015). Recent advances in lipase-mediated preparation of pharmaceuticals and their intermediates. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 16(12), 29682-29716 [10.3390/ijms161226191].

Recent advances in lipase-mediated preparation of pharmaceuticals and their intermediates

Serra I.
2015

Abstract

Biocatalysis offers an alternative approach to conventional chemical processes for the production of single-isomer chiral drugs. Lipases are one of the most used enzymes in the synthesis of enantiomerically pure intermediates. The use of this type of enzyme is mainly due to the characteristics of their regio-, chemo- and enantioselectivity in the resolution process of racemates, without the use of cofactors. Moreover, this class of enzymes has generally excellent stability in the presence of organic solvents, facilitating the solubility of the organic substrate to be modified. Further improvements and new applications have been achieved in the syntheses of biologically active compounds catalyzed by lipases. This review critically reports and discusses examples from recent literature (2007 to mid-2015), concerning the synthesis of enantiomerically pure active pharmaceutical ingredients (APIs) and their intermediates in which the key step involves the action of a lipase.
Articolo in rivista - Review Essay
Biocatalysis; Enantioselectivity; Kinetic resolution; Lipases; Pharmaceuticals;
English
2015
16
12
29682
29716
none
Carvalho, A., Fonseca, T., De Mattos, M., De Oliveira, M., De Lemos, T., Molinari, F., et al. (2015). Recent advances in lipase-mediated preparation of pharmaceuticals and their intermediates. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 16(12), 29682-29716 [10.3390/ijms161226191].
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Utilizza questo identificativo per citare o creare un link a questo documento: https://hdl.handle.net/10281/316430
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