Three-component cyclization of hydroxylamino-substituted quinoline with reactive methylene compounds and formaldehyde: new method for the synthesis of 7-(isoxazolidin-2-yl)-6-fluoroquinolones

A one-step procedure was developed for the synthesis of new 6-fluoro-7-(isoxazolidin-2-yl)-4-oxo-1,4-dihydroquinolines. The procedure is based on the 1,3-dipolar cycloaddition of the azomethine oxide and 1,1-disubstituted alkenes, which are generated in situ from 6-fluoro-7-hydroxylamino-4-oxo-1,4-dihydroquinoline-3-carboxylic acid and CH-active compounds (dialkyl malonates, ethyl acetoacetate), respectively, in the presence of formaldehyde at 100—120 °C.     

Fluorinated 1,3-benzothiazin-4-ones containing fluoroquinolone fragment

Chemistry of Heterocyclic Compounds - We have developed an efficient synthetic approach to potential antibacterial agents with double mechanism of action through the combination of antibacterial...     

MnO2-Mediated Oxidative Cyclization of “Formal” Schiff’s Bases: Easy Access to Diverse Naphthofuro-Annulated Triazines

A different type of MnO₂-induced oxidative cyclization of dihydrotriazines has been developed. These dihydrotriazines are considered as a “formal” Schiff’s base. This method provided easy access to naphthofuro-fused triazine via the C-C/C-O oxidative coupling reaction. The reaction sequence comprised the nucleophilic addition of 2-naphthol or phenol to 1,2,4-triazine, followed by oxidative cyclization. The scope and limitations of this novel coupling reaction have been investigated. Further application of the synthesized compound has been demonstrated by synthesizing carbazole-substituted benzofuro-fused triazines. The scalability of the reaction was demonstrated at a 40 mmol load. The mechanistic study strongly suggests that this reaction proceeds through the formation of an O-coordinated manganese complex.     

Antiviral Agents – Benzazine Derivatives

Chemistry of Heterocyclic Compounds - The review outlines the results of studies of the antiviral activity of quinoline, quinoxaline, and quinazoline derivatives published over the past 5 years....