Abstract::
This study aims to develop a practical and facile one-pot synthesis of 2-
substituted quinazolines. Using a commercially available and structurally simple ruthenium(
II) complex as the catalyst to synthesize a series of quinazoline derivatives via acceptorless
dehydrogenative coupling. The mechanism of this reaction was explored by control
reaction and DFT calculation. This protocol offers access to a diverse array of quinazoline
derivatives (52 examples) in moderate to excellent yields (29%-98%). In summary, we
have developed an efficient one-pot ruthenium (II)-catalyzed ADC synthesis of quinazoline
under an air atmosphere. The reaction only produces hydrogen and water as by-products,
serving as a sustainable and atom-efficient synthetic approach.