Access to enantioenriched dihydroquinoxalinones via Cu-catalyzed propargylic substitution

We report herein a copper-catalyzed straightforward approach for the synthesis of otherwise synthetically challenging enantioenriched dihydroquinoxalinones from propargylic esters and commercially readily available o-phenylenediamines. This catalytic approach could be performed open to air on a gram-scale, with the reaction efficiency being unaffected. The dangling propargylic substituent in the products could be transformed into different functional groups with easy operation, therefore creating much potential for structural diversity.