The parallel solution-phase synthesis of more than 2200 7-trifluoromethyl-substituted pyrazolo[1,5-a]pyrimidine and 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrimidine carboxamides on a 50-100-mg scale has been accomplished. Key reactions include assembly of the pyrazolo[1,5-a]pyrimidine ring by condensation of 5-aminopyrazole derivatives with the corresponding trifluoromethyl-beta-diketones. The libra...

A one-pot three-component synthesis of dihydropyrimidinones via a molecular iodine-catalyzed tandem reaction of simple readily available mono-substituted urea, alkylaldehyde, and arylaldehyde has been developed. The reaction proceeds with high chemo- and regioselectivity to give highly diverse dihydropyrimidinones in reasonable yields under mild reaction conditions. Moreover, the first catalyti...

A water-soluble furyl-substituted diarylethene derivative has been prepared that can undergo reversible Diels-Alder reactions with maleimides to yield photoswitchable Diels-Alder adducts. Employing bioorthogonal visible light, the release of therapeutically effective concentrations of maleimide-based reactive inhibitors or labels from these "prodrugs" or "protags" could be photoreversibly trigg...

A novel ferrocene substituted PDA (FEPDA) material was synthesized and its chromatic phase transition behavior was studied under the application of a negative bias voltage. By the combination with CMS techniques, FEPDA materials could be used as a probe for mapping the topographic carrier density distribution in organic devices.

New carborane anions carrying one or three triflyloxy substituents are described. The mono-triflyloxy substituted carborane can be halogenated to give pentabromo and decachloro derivatives with preservation of the B-OTf linkage. The use of [HCB11Cl10OTf](-) as a weakly coordinating anion is demonstrated.

The on-going need for feature miniaturization and the growing complexity of structures for use in nanotechnology demand the precise and controlled formation of covalent bonds at the molecular level. Such control requires the use of external stimuli that offer outstanding spatial, temporal, as well as energetic resolution. Thus, photoaddressable switches are excellent candidates for creating a s...

A series of 3,5-bis(hetero)arylethenyl-substituted BODIPY derivatives have been prepared by Knoevenagel-type condensation alkyl-substituted with the corresponding aldehydes. 2-Pyrrolylethenyl-substituted feature near-IR emission (?em > 700 nm) a high fluorescence quantum yield. Both maxima and yields are relatively insensitive to solvent polarity, contrary near-IR-emitting 4-(N,N-dimethylaminop...

Second-order rate constants (kN) have been measured spectrophotometrically for the nucleophilic displacement reactions of 4-nitrophenyl X-substituted-cinnamates (4a-4e) and Y-substituted-phenyl cinnamates (5a-5e) with Z-substituted-phenoxide anions in 80 mol % H2O/20 mol % DMSO at 25.0 ± 0.1 C. The Hammett plot for the reactions of 4a-4e with 4-chlorophenoxide (4-ClPhO) consists of two intersec...

novel analogues of n-piperazinyl fluoroquinolones were prepared and evaluated against a panel of gram-positive and gram-negative bacteria, to study the effect of introducing bulky anthracene and phenanthrene moieties on the antibacterial effects of norfloxacin, ciprofloxacin and gatifloxacin. although most of the novel synthesized compounds had lower antibacterial effects, some derivatives show...

Novel analogues of oxadiazole-substituted naphtho[2,3-b]thiophene-4,9-diones were synthesized in which the tricyclic quinone skeleton was systematically replaced with simpler moieties, such as structures with fewer rings and open-chain forms, while the oxadiazole ring was maintained. In addition, variants of the original 1,2,4-oxadiazole ring were explored. Overall, the complete three-ring quin...