Copper-catalyzed dehydrogenative γ-C(sp³)-H amination of saturated ketones for synthesis of polysubstituted anilines.

ABSTRACT: Metal-catalyzed β-C-H functionalization of saturated carbonyls via dehydrogenative desaturation proved to be a powerful tool for simplifying synthesis of valuable β-substituted carbonyls. Here, we report a copper-catalyzed dehydrogenative γ-C(sp³)-H amination of saturated ketones that initiates the three-component coupling of saturated ketones, amines and N-substituted maleimides to construct polysubstituted anilines. The protocol presented herein enables both linear and α-branched butanones to couple a wide spectrum of amines and various N-substituted maleimides to produce diverse tetra- or penta-substituted anilines in fair-to-excellent yields with good functional group tolerance. The mechanism studies support that this ketone dehydrogenative γ-C(sp³)-H amination wa

SUBMITTER: Hu R 

PROVIDER: S-EPMC6695438 | biostudies-literature | 2019 Aug

REPOSITORIES: biostudies-literature