Abstract
Considering oxatriazino[a]isoindole as a wealthy structure for developing molecules of impressive therapeutic potentials, some new oxatriazino[3,2‐a]isoindoles analogs were synthesized. Thus, 3‐mercapto‐6H‐[1,2,4,5]oxatriazino[3,2‐a]isoindol‐6‐one (5), was prepared as one‐pot three‐components product and subjected to a series of manipulations including cycloaddition reactions to annulate a series of pharmacophoric motif conjugates. The structures of the newly synthesized compounds were elucidated based on their correct elemental and spectroscopic data.