Novel oxazolidin-2-one-linked 1,2,3-triazole derivatives () were synthesized by straightforward and versatile azide-enolate (3 + 2) cycloaddition. The series of compounds was screened for antifungal activity against four filamentous fungi as well as six yeast species of spp. According to their efficiency and breadth of scope, they can be ordered as > > > , especially in relation to the activity displayed against ATCC-34138, ATCC-28592 and ATCC-8690, compounds, and showed excellent activity against (MIC 0.12, 0.25 and 0.12 μg mL, respectively), better than that of itraconazole (MIC 1 μg ml). The activity of compound (MIC = 2 μg mL) was higher than that observed for the standard antifungal drug (MIC = 8 μg mL) against , while compound displayed an excellent antimycotic activity against (MIC = 2 μg mL 4 μg mL for itraconazole). In addition, we describe herein a novel mild and eco-friendly synthetic protocol for obtaining β-ketosulfones (adducts to afford compounds ) from α-brominated carbonyls in an aqueous nanomicellar medium at room temperature.
A multicomponent diversity-oriented synthesis of new highly emissive tetracyclic isoquinolines that target specific organelles is described. The title compounds were prepared via a three-step protocol starting with an Ugi fourcomponent reaction, followed by either an intramolecular alkyne hydroarylation and subsequent alkene isomerization or through a Pomeranz−Fritsch-type cyclization with a final intramolecular Heck reaction. Subcellular localization studies of these compounds using green channel confocal microscopy revealed remarkable and distinctive distribution patterns in live cells, showing an unprecedented high selectivity and imaging contrast. The differentiated organelle visualizationincluding localizers for mitochondria, lysosomes, Golgi apparatus, endoplasmic reticulum, and plasma membranewas achieved by varying the nature of the tetracyclic system and substituent pattern, changing the original four-component set in the starting Ugi reaction.
A continuous flow method for the selective reduction of aromatic nitriles to the corresponding amine is reported. The method is based on a ruthenium-catalysed transfer-hydrogenation process, requires no additives, and uses isopropanol as both solvent and reducing agent. The process utilizes 1 mol% of the commercially available [Ru(
p
-cymene)Cl
2
]
2
, with a residence time of ca. 9 min, and a throughput of 50 mmol/h. The method was successfully applied to a range of aromatic nitriles providing the corresponding primary amines in good yields.
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