The synthesis of highly substituted imidazole derivatives has been achieved from various α-azido chalcones, aryl aldehydes, and anilines. This multicomponent protocol employs erbium triflate as a catalyst resulting in excellent yield of the imidazoles.

An efficient synthesis of 3-substituted-5-arylamino-1,2,4-thiadiazoles through intramolecular oxidative S-N bond formation of imidoyl thioureas by phenyliodine(III) bis(trifluoroacetate) is reported. The protocol features a metal-free approach, broad substrate scope, very short reaction times, good to excellent yields, and simple starting materials.

We report a single‐molecule radiotracer that can be labeled independently with 18F‐fluoride or radiometals (64Cu, 177Lu) in a single step. A prostate‐specific membrane antigen (PSMA)‐targeting ligand, armed with both an organotrifluoroborate and a metal‐chelator (DOTA), was designed to optionally afford 18F‐, 64Cu‐ or 177Lu‐labeled products that were injected into mice bearing prostate cancer (LNCaP) xenografts. PET/CT images and ex vivo biodistribution data show high, specific tumor uptake irrespective of which radionuclide is used, thereby demonstrating a new approach to combining, in a single molecule, 18F‐labeling capabilities for PET imaging with radiometalation for potential imaging and therapeutic applications.

The synthesis of boranil dye fluorescent probes for the detection of hydrogen peroxide has been described. The probes have been successfully applied for imaging of H2O2 in HeLa cells under physiological conditions.

A divergent reactivity of α-azidochalcones with metal β-diketonates for the synthesis of substituted pyrroles and indoles is described.

The copper(II)‐catalyzed C–S cross coupling of thiazolidine‐2‐thiones with organoboronic acids towards the synthesis of azole sulfides was investigated. This mild and base‐free protocol has the advantages of short reaction times and excellent yields with no need for an ancillary ligand.

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SummaryThe reaction of α-azidochalcones with carboxylic acids has been investigated resulting in the formation of α-amido-1,3-diketones under microwave irradiation via in situ formation of 2H-azirine intermediates. An interesting reaction is described wherein, with trifluoroacetic acid at lower temperature, it affords highly substituted 2-(trifluoromethyl)oxazoles. These flexible transformations proceed under solvent free conditions in good to excellent yields without any catalyst.