Site-Selective Palladium(II)-Catalyzed Methylene C(sp3)-H Diarylation of a Tropane Scaffold.

A series of 2,4-di-arylated tropane derivatives was synthesized through a site-selective palladium-catalyzed ß-C(sp3)-H di-arylation process. This type of structure has been scarcely reported in literature. They nevertheless represent an interesting class of biologically relevant molecules as illustrated by the observed activity at the micromolecular level of eight derivatives toward human colorectal cancer cell line HCT116.