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.

RESUMO: "Constituintes químicos e atividade antioxidante de duas variedades de água de coco (Cocos nucifera L.)". Uma análise dos componentes da água-de-coco (Cocos nucifera L.) de duas variedades da fruta (verde e amarelo) por hidrodestilação e extração com solvente, mostrou a presença de álcoois, cetonas, tióis, ácidos carboxílicos, fenóis, e ésteres. Significativa atividade antioxidante foi observada, usando o método DPPH, para as amostras obtidas por hidrodestilação e extração de éter de petróleo para ambas as variedades do coco. Unitermos:Cocos nucifera, Arecaceae, água-de-coco, composição química, atividade antioxidante.ABSTRACT: An analysis of the constituents of coconut (Cocos nucifera L.) water from two fruit varieties (green and yellow) by hydrodistillation and solvent extraction showed the presence of alcohols, ketones, thiols, carboxylic acids, phenols, and esters. Substantial antioxidant activity was observed, using the DPPH assay, for the samples obtained by hydrodistillation and petroleum ether extraction of both coconut varieties.

A convenient synthesis of the new enamine derivatives 2-(4-morpholinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione, 2-(1-piperidinyl)-3-(3-methyl-2-butenyl)-1,4-naphtalenedione and 2-(1-pyrrolidinyl)-3-(3-methyl-2-butenyl)-1,4-naphthalenedione was carried out from natural 2-hydroxy-3-(3-methyl-2-butenyl)-1,4-naphthalenedione (lapachol) and morpholine, piperidine and pyrrolidine. The structures of the products were established mainly by NMR analysis, including 2D experiments. Biological activities of these products were evaluated against Artemia salina, Aedes aegypti and cytotoxicity using A549 human breast cells.

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