Abstract Dihydroimidazo [5, 1-c][1, 2, 4] triazine-3, 6 (2H, 4H)-dione derivatives were prepared by successive N3-and N1-alkylation of hydantoins, followed by regioselective thionation and subsequent cyclization under mild conditions. In a final alkylation step a further substituent may be introduced. The synthetic strategy allows broad structural variation of this new drug-like heterobicyclic scaffold. In addition to extensive NMR and ...