Palladium-Catalyzed Dearomative syn-1,4-Carboamination

A dearomative 1,4-carbo­amination of arenes has been achieved using areno­phile cycloaddition and subsequent palladium-catalyzed substitution with non­stabilized lithium enolates. This protocol delivers products with exclusive syn-1,4-selectivity and can be also conducted in an asymmetric fashion. The method allows rapid dearomative difunctionalization of simple aromatic compounds into functional small molecules amenable to further diversification.