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Int. J. Mol. Sci. 2015, 16(12), 29682-29716; doi:10.3390/ijms161226191

Recent Advances in Lipase-Mediated Preparation of Pharmaceuticals and Their Intermediates

1
Laboratório de Biotecnologia e Síntese Orgânica (LABS), Department of Organic and Inorganic Chemistry, Federal University of Ceará, Campus do Pici, Postal box 6044, 60455-970 Fortaleza, Ceará, Brazil
2
Department of Food, Environmental and Nutritional Sciences (DEFENS), University of Milan, via Mangiagalli 25, 20133 Milan, Italy
*
Author to whom correspondence should be addressed.
Academic Editor: Vladimír Křen
Received: 28 October 2015 / Revised: 4 November 2015 / Accepted: 4 November 2015 / Published: 11 December 2015
(This article belongs to the Special Issue Molecular Biocatalysis)

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. View Full-Text
Keywords: biocatalysis; lipases; kinetic resolution; enantioselectivity; pharmaceuticals biocatalysis; lipases; kinetic resolution; enantioselectivity; pharmaceuticals
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This is an open access article distributed under the Creative Commons Attribution License which permits unrestricted use, distribution, and reproduction in any medium, provided the original work is properly cited. (CC BY 4.0).

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MDPI and ACS Style

Carvalho, A.C.L.M.; Fonseca, T.S.; Mattos, M.C.; Oliveira, M.C.F.; Lemos, T.L.G.; Molinari, F.; Romano, D.; Serra, I. Recent Advances in Lipase-Mediated Preparation of Pharmaceuticals and Their Intermediates. Int. J. Mol. Sci. 2015, 16, 29682-29716.

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