Moclobemide is a selective and reversible monoamine oxidase-A inhibitor, which is used as an antidepressant. Three moclobemide analogues were synthesized by replacing moclobemide phenyl ring with substituted imidazoles. So, N-[(4-morpholinyl) ethyl)]-1-benzyl-2-(alkylthio)-1H-imidazole-5-carboxamides (7a-c) were synthesized and studied for the antidepressant activity using forced swimming test ...

A new mechanistic approach for the catalytic, enantioselective conjugate addition of nitrogen-based nucleophiles to acceptor-substituted alkenes is reported, which is based on a visible light induced and phosphate base promoted transfer of a single electron from a nitrogen nucleophile to a catalyst-bound acceptor-substituted alkene, followed by a stereocontrolled C-N bond formation through ster...

Quaternisation of 3,5-diaryl-1,2,4-thiadiazoles with trimethylsilylmethyl triflate at 40 8C occurred at N-2. Separate desilylation of the salts resulted in a ring expansion to substituted 2H-1,3,5-thiadiazines 5. Heating of these with ethanolic sodium ethoxide caused sulfur extrusion and ring contraction to 2,4-disubstituted imidazoles 6. 3,4-Diaryl1,2,5-thiadiazoles were less reactive to alkyl...

Oxidation of substituted imidazoles with modified Fenton's reagent (Fe(II), ascorbic acid, EDTA and H2O2) in aqueous solution at pH 5 -7 in the presence of inorganic orthophosphate gives high yields of an unknown bound phosphate, in the case of 2-methylimidazole up to 3 5 % based on inorganic phosphate. The dependence of the yields on reaction parameters and the hydrolytic behaviour of the comp...

We describe here a tandem catalytic route to prepare imidazoles in a single operation from aryl iodides, imines and CO. The reaction involves a catalytic carbonylation of aryl halides with imines to form 1,3-dipoles, which undergo spontaneous 1,3-dipolar cycloaddition. Overall, this offers an alternative to coupling reactions to construct the (hetero)aryl-imidazole motif, where variation of the...