The total synthesis of the plant natural product altissimacoumarin D was achieved by the Mitsunobu alkylation of isofraxidin by geraniol. Isofraxidin was prepared from 2,4-dihydroxybenzaldehyde in five steps. The key reaction was the Knoevenagel condensation of an ortho-hydroxybenzaldehyde with Meldrum's acid under neutral conditions in water and one-pot acid catalyzed cyclization to the coumarin.

A suitable and efficient high-performance liquid chromatography (HPLC) method was developed for the simultaneous determination of tuberculostatic isoniazid and its related impurities, isonicotinic acid and isonicotinamide, in oral solid dosage forms. We studied the influence on chromatographic separation of mobile phase parameters, such as pH, ion pairing and ionic strength, as well as column bonded phase and brands. The use of buffer solution pH 6.8:acetonitrile 96:4 (v/v) at 0.8 mL min-1, C18 column (250 × 4.6 mm, 5 µm), allowed proper separation of these ionizable analytes without the need of ion pairing agents. The limit of quantification of the method (0.1 µg mL-1) was suitable for the analysis of impurities. A drug-excipient compatibility study was carried out with the anaytical method proposed in this work and addressed frequent excipients used in isoniazid coated tablets. The dye FD&C blue 2 lake promoted the highest degradation of the tuberculostatic agent.

AbstractThis paper presents a technological innovation that uses a subclass of glycerophospholipids as a booster biocide in antifouling paint. These glycerophospholipid PAF-analogs are economically and environmentally viable compounds because they are synthesized from a metal-free raw material source-soybean lecithin. The synthesis, which involves transesterification followed by an alkylation reaction, produced a mixture of glycerophospholipids that were characterized by mass spectrometry. Evaluation of the antifouling performance with field tests showed that the replacement of ordinary halogenated booster biocide with the synthesized product gave a better efficiency and an exceptional antifouling activity with a significant reduction in the coverage of the fouling macro-organisms.

In this work we describe a new efficient strategy for the preparation of 1,2,4-trimethoxybenzene (3) in 56% overall yield. The compound 3 was used in a preliminary study of insect attraction by a mixture of semiochemicals called TIV, composed of indol (1), vanillin (2) and 1,2,4-trimethoxybenzene (3), in eight Mc Phail style traps installed at a domestic orchard of citric-culture, containing 120 trees not infected by plagues in Bom Jesus Farm, located next to a patch of the Atlantic Forest, at Silva Jardim, Rio de Janeiro, Brazil.

Several methodologies concerning the preparation of 2-aryl and 2-heteroarylcyclohexanones are presented. The use of these intermediates in the synthesis of chemically and biologically interesting organic compounds is also discussed.