title: Recent Advances in Lipase-Mediated Preparation of Pharmaceuticals and Their Intermediates.
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.
authors.affiliation: 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. carol.luz@hotmail.com.
authors.forename: Ana Caroline Lustosa de Melo
authors.initials: AC
authors.lastname: Carvalho
authors.affiliation: 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. thiagofonseka@hotmail.com.
authors.forename: Thiago de Sousa
authors.initials: Tde S
authors.lastname: Fonseca
authors.affiliation: 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. mcdmatto@ufc.br.
authors.forename: Marcos Carlos
authors.initials: MC
authors.lastname: de Mattos
authors.affiliation: 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. mcfo@ufc.br.
authors.forename: Maria da Conceição Ferreira
authors.initials: Mda C
authors.lastname: de Oliveira
authors.affiliation: 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. tlemos@dqoi.ufc.br.
authors.forename: Telma Leda Gomes
authors.initials: TL
authors.lastname: de Lemos
authors.affiliation: Department of Food, Environmental and Nutritional Sciences (DEFENS), University of Milan, via Mangiagalli 25, 20133 Milan, Italy. francesco.molinari@unimi.it.
authors.forename: Francesco
authors.initials: F
authors.lastname: Molinari
authors.affiliation: Department of Food, Environmental and Nutritional Sciences (DEFENS), University of Milan, via Mangiagalli 25, 20133 Milan, Italy. diego.romano@unimi.it.
authors.forename: Diego
authors.initials: D
authors.lastname: Romano
authors.affiliation: Department of Food, Environmental and Nutritional Sciences (DEFENS), University of Milan, via Mangiagalli 25, 20133 Milan, Italy. Immacolata.serra@unimi.it.
authors.forename: Immacolata
authors.initials: I
authors.lastname: Serra
mesh_terms: D000818:Animals; D055162:Biocatalysis; D060326:Chemistry Techniques, Synthetic / Q000379:methods*; D004795:Enzyme Stability; D004951:Esterification; D006801:Humans; D006868:Hydrolysis; D008049:Lipase / Q000737:chemistry* / Q000378:metabolism; D004364:Pharmaceutical Preparations / Q000138:chemical synthesis*
chemical_list: D004364:Pharmaceutical Preparations; D008049:Lipase
keywords: biocatalysis; enantioselectivity; kinetic resolution; lipases; pharmaceuticals