No abstract

Our data demonstrated lithium-mimetic effects of ebselen in different experimental models of 5-HT receptor function, probably mediated by IMPase inhibition. This evidence of lithium-like neuropharmacological effects of ebselen adds further support for the clinical testing of ebselen in mood disorders, including as an antidepressant augmenting agent.

Markieren leicht gemacht: Der Austausch einer hoch fluorierten Sulfonatmarkierung gegen [18F]‐Fluorid erwies sich als vorteilhaft für die Erzeugung 18F‐markierter prosthetischer Gruppen und bekannter Radiotracer (siehe Bild). Eine fluorige Festphasenextraktion (FSPE) trennte den Überschuss der hoch fluorierten Vorstufe vom markierten Material, sodass auf eine Destillation oder andere aufwändige Trennverfahren verzichtet werden kann.

Two routes are described for the synthesis of the sawaranospirolides, stereoisomeric spirolactone ascorbigenins isolated from Chamaecyparis pisifera. Trapping of the keto enal formed by oxidation of a functionalised 2-(4-hydroxybutyl)furan affords a potential butenolide spiroacetal precursor to sawaranospirolides A and C. Alternatively, epoxidation of protected 3-(dihydropyran-2-yl)-3-arylpropanoic acids results in spirolactonisation to generate ent-sawaranospirolide C; a related acid-mediated spirocyclisation gave access to ent-sawaranospirolide D.

The synthesis is described of a range of 3-alkylidene-2-oxabicyclo[2.2.1]hept-5-ene and 3-alkylidene-2-oxabicyclo[2.2.2]oct-5-ene derivatives; Claisen rearrangement of these substrates either thermally or in the presence of an added Lewis acid results in the formation of bicyclic cyclobutanones with generally good conversions. These reactions may be performed in hydroxylic solvents, supporting a largely non-dissociative pathway for the rearrangement.