Trioxanes 8a–b, easily accessible in two steps from allylic alcohol 6a–b, on reductive amination with 4-aminoquinolines 4a–c furnish a new series of trioxaquines 9a–b, 10a–b, 11a–b in 32–77% yields. Dicitrate salts of these trioxaquines have been evaluated for antimalarial activity against multidrug resistant Plasmodium yoelii in mice model.