A copper-catalyzed regio- and intermolecular aminofluorination of styrenes has been developed. In this reaction Ph-I=N-Ts and Et3N·3HF act as nitrogen and fluorine sources, respectively. The obtained β-fluoro-N-Ts-phenethylamines can be N-alkylated with subsequent deprotection affording the corresponding β-fluoro-N-alkylated phenethylamines, which are interesting building blocks for compounds a...

Density functional theory computations with dispersion corrections (DFT-D) were performed to investigate the dihalogen interactions and their effect on the electronic band structures of halogenated (fluorinated and chlorinated) BN bilayers and aligned halogen-passivated zigzag BN nanoribbons (BNNRs). Our results reveal the presence of considerable homo-halogen (FF and ClCl) interactions in bila...

7-O-[2,6-Dideoxy-2-fluoro-4-O-(3-fluorotetrahydropyran-2-yl)-alpha -L- talopyranosyl]daunomycinones (7a-7c) have been prepared by condensation of 3'-O-benzoyl derivative of 7-O-(2,6-dideoxy-2-fluoro-alpha-L-talopyranosyl)daunomycinone with 2,3-difluorotetrahydropyran as the key reaction. Antitumor activities of these compounds are described.

The fluorescent agent Fluoro Jade was applied to cortical brain sections obtained from human patients at early postnatal ages and in patients with Alzheimer's disease, and from a Cebus apella monkey after mechanical lesioning of the cerebral cortex. Fluoro Jade labeled reactive astrocytes and early differentiating astroglial cells.

3-Fluoro- and trifluoromethylthio-piperidines represent important building blocks for discovery chemistry. We report a simple efficient method to access analogs of these compounds that are armed with rich functionality allowing them be chemoselectively derivatized high diastereocontrol.

In the crystal structure of the title compound, C(18)H(11)FN(4), the pyridopyrazine ring makes dihedral angles of 34.67 (7) and 52.24 (7)° with the 4-fluoro-phenyl and pyridine rings, respectively. The 4-fluoro-phenyl ring makes a dihedral angle of 59.56 (9)° with the pyridine ring.

Radical-mediated thiodesulfonylation of the vinyl and (α-fluoro)vinyl sulfones, derived from aldehydes and ketones, with aryl thiols in organic or aqueous medium provided access to vinyl and (α-fluoro)vinyl sulfides. The vinyl sulfides were formed predominantly with E stereochemistry independent of the stereochemistry of the starting vinyl sulfones.

α-Fluoro-α-nitro esters were used as reaction partners in Michael addition to nitroalkenes, and the products were obtained in excellent chemical yields and with high enantioselectivities. Moreover, α-fluoro-α-amino ester with a quaternary α-carbon was prepared for the first time.

A practical synthesis of the Rho-Kinase inhibitor Y-27632 and two new fluoro derivatives was achieved in seven steps and with a good overall yield of 45% starting from commercially available (R)-1-phenylethylamine. Compared to Y-27632 the new fluoro derivatives showed reduced or no effect on hPSC vitality and expansion after dissociation in human pluripotent stem cells.

Concentration jump responses to 5-substituted (S)-willardiines were recorded from dorsal root ganglion (DRG) and hippocampal neurons under voltage clamp. After block of desensitization by concanavalin-A, dose-response analysis for activation of kainate-preferring receptors in DRG neurons gave the potency sequence trifluoromethyl > iodo > bromo approximately chloro > nitro approximately cyano > ...