Abstract
A Brønsted acid-catalyzed peroxidation of 3-hydroxyisoindolinones with hydroperoxides has been established for the first time, which constructs α-amino peroxides bearing a tetrasubstituted stereocenter in good to high yields and enantioselectivities. The transformation uses of environmentally benign solvents, and features operational simplicity, and high atom economy. The synthetic utility was demonstrated with the gram-scale reactions and further transformations of the products. Notably, preliminary bioactivity studies reveal that these valuable α-amino peroxides show potential anticancer activity.
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