Dimethylformamide (DMF) acts as an efficient source of carbon monoxide and dimethylamine in the palladium-catalyzed aminocarbonylation (Heck carbonylation) of p-tolyl bromide to provide the dimethylamide. Addition of amines to the reaction mixture in excess delivers the corresponding aryl amides in good yields. The amines employed, benzylamine, morpholine, and aniline, all constitute good react...

The direct and catalytic incorporation of fluorine containing molecular motifs into organic compounds resulting high-value added chemicals represents a rapidly evolving part synthetic methodologies, thus this area is in the focus pharmaceutical agrochemical research. Herein we report stereoselective procedure for fluorovinylation aromatic heteroaromatic scaffolds. This methodology development h...

A systematic study of the structure-activity relationships of 2b (OL-135), a potent inhibitor of fatty acid amide hydrolase (FAAH), is detailed targeting the C2 acyl side chain. A series of aryl replacements or substituents for the terminal phenyl group provided effective inhibitors (e.g., 5c, aryl = 1-napthyl, Ki = 2.6 nM), with 5hh (aryl = 3-ClPh, Ki = 900 pM) being 5-fold more potent than 2b...

While 3 parent carcinogens, namely AAF-2,2 dibenz (a,h) anthracene, and N-acetyl-4-aminobiphenyl3 did not expose a mitochondrial thiol group, appropriate acidic metabolites of these carcinogens did expose a mitochondrial thiol group (6, 7, 9). In orderto examine thisconfluence further, we have experimented with AAF-2 and some of its isomers, namely, N-OH-AAF4, have also been examined (Chart 1)....

Studies on the palladium-catalyzed formation of aryl amines, aryl ethers and a-aryl carbonyl compounds from aryl halides are reported. These studies range from synthetic methodology, to detailed mechanistic analysis, to new methods one can use to screen for catalytic covalent bond formation. Improved methods for formation of aryl ethers and room temperature amination chemistry have resulted fro...