Efficient three-step synthesis of benzo[<i>e</i>]imidazo[1,2-<i>c</i>][1,2,3]triazines

<p>A novel three-step sequence toward benzo[<i>e</i>]imidazo[1,2-<i>c</i>][1,2,3]triazine derivatives is investigated. This pathway started from commercially available starting materials afforded <b>5a–h</b> in good to excellent yields. In this method, we took the advantage of diazonium chemistry, which was followed by intramolecular N-N bond formation in the construction of N-rich cycles.</p

An efficient, four-component reaction for the synthesis of novel carbamodithioates

<p>A series of substituted phenylcarbamoyl methyl benzylcarbamodithioates have been synthesized using the multicomponent condition. The reaction proceeded under mild practical condition and afforded the desired products in good yields.</p

Straightforward Approach Toward Dihydrothiazoles via Intramolecular Bromocyclization

<div><p></p><p>An intramolecular bromonium ion–assisted cyclization with sulfur as an internal nucleophile is described. Starting from benzoyl chlorides, this method provides an easy procedure for the synthesis of dihydrothiazole derivatives in moderate to good yields.</p></div

Quinoline-based imidazole-fused heterocycles as new inhibitors of 15-lipoxygenase

<p>A series of 2-chloro-quinoline-based imidazopyridines <b>6a–l</b> and imidazothiazoles <b>6m–o</b> bearing a bulky alkylamine side chain were synthesized as soybean 15-LOX inhibitors. The target compounds <b>6a–o</b> were prepared <i>via</i> one-pot reaction of 2-chloroquinoline-3-carbaldehyde (<b>3</b>), heteroaromatic amidine <b>4</b>, and alkyl isocyanides <b>5</b>, in the presence of NH₄Cl. All compounds showed significant anti-15-LOX activity (IC₅₀ values ≤40 μM). Among the title compounds, the imidazo[2,1-<i>b</i>]thiazole derivative <b>6n</b> bearing a <i>tert</i>-butylamine moiety showed the highest activity against soybean 15-LOX enzyme.</p