An experimental and theoretical study of reaction mechanisms between nitriles and hydroxylamine.

The industrially relevant reaction between nitriles and hydroxylamine yielding amidoximes was studied in different molecular solvents and in ionic liquids. In industry, this procedure is carried out on the ton scale in alcohol solutions and the above transformation produces a significant amount of unexpected amide by-product, depending on the nature of the nitrile, which can cause further analytical and purification issues. Although there were earlier attempts to propose mechanisms for this transformation, the real reaction pathway is still under discussion.

Evaluation of SSR161421, a novel orally active adenosine A3 receptor antagonist on pharmacology models.

The effects of a novel adenosine A(3) receptor antagonist, SSR161421, were examined on both antigen per se and adenosine receptor agonist-increased airway responses in antigen-sensitized guinea pigs. Adenosine (10(-5)M) and AB-MECA [N6-(4-aminobenzyl)-adenosine-5'-N-methyl-uronamide dihydrochloride] (10(-7)M) increased the antigen response up to 61 ± 3.0% and 88 ± 5.

Interaction of SSR161421, a novel specific adenosine A(3) receptor antagonist with adenosine A(3) receptor agonists both in vitro and in vivo.

A novel adenosine A(3) receptor antagonist (SSR161421) was characterized by both receptor binding assays and pharmacological tests. Binding studies on cloned human adenosine receptors showed that SSR161421 has high affinity for adenosine hA(3) receptors (K(i)=0.37 nM) with at least 1000-fold selectivity compared to hA(1), hA(2A) and hA(2B) receptors.

Design and application of new imidazolylsulfonate-based benzyne precursor: an efficient triflate alternative.

Several o-(trimethylsilyl)aryl imidazolylsulfonates were synthesized in a simple process and successfully applied in cycloadditions involving benzyne intermediates. The precursor offers an efficient alternative for generating benzynes compared to widely used ortho TMS triflates under similar reaction conditions. With the utilization of this new precursor, the formation of potentially genotoxic trifluoromethanesulfonate side product is eliminated.

Dual luminescence properties of differently benzo-fused N-phenylphenanthridinones.

The photophysics of some newly prepared N-arylphenanthridinone derivatives have been investigated. It has been demonstrated how the luminescence properties are influenced by the size of the aromatic ring system. It has been shown that the replacement of the phenyl group in N-phenyphenanthridinone (PP) by an alpha-naphthyl or beta-naphthyl group (alphaNP and betaNP, respectively), influences the fluorescence spectra very differently.

Valence Bond Isomerization of Fused [1,2,3]Triazolium Salts with Bridgehead Nitrogen Atom. Fused Azolium Salts. 19(,).

[1,2,3]Triazolo[1,5-a]quinolinium (7), [1,2,3]triazolo[1,5-b]isoquinolinium (8), and [1,2,3]triazolo[1,5-a]pyrazinium salts (9) when heated in trifluoroacetic acid and/or 1,2-dichlorobenzene undergo valence bond isomerization to ring-opened reactive intermediates (e.g., 8 gave 13) which can participate in (i) electrophilic substitution as nitrenium cations to yield pyrazole- and indazole-fused new heterocycles (e.