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.
Recent Advances in Lipase-Mediated Preparation of Pharmaceuticals and Their Intermediates / A.C. Lustosa de Melo Carvalho, T. de Sousa Fonseca, M.C. de Mattos, M. Ferreira de Oliveira, T.L. Gomes de Lemos, F. Molinari, D. Romano, I. Serra. - In: INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES. - ISSN 1422-0067. - 16:12(2015 Dec), pp. 29682-29716. [10.3390/ijms161226191]
Recent Advances in Lipase-Mediated Preparation of Pharmaceuticals and Their Intermediates
F. Molinari;D. RomanoPenultimo
;I. SerraUltimo
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.File | Dimensione | Formato | |
---|---|---|---|
ijms-16-26191-v2.pdf
accesso aperto
Tipologia:
Publisher's version/PDF
Dimensione
7.11 MB
Formato
Adobe PDF
|
7.11 MB | Adobe PDF | Visualizza/Apri |
Pubblicazioni consigliate
I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.