A Dual-Catalytic Strategy To Direct Asymmetric Radical Aminotrifluoromethylation of Alkenes

A novel asymmetric radical aminotrifluoromethylation
of alkenes
has been developed for the first time, providing straightforward access
to densely functionalized CF3-containing azaheterocycles
bearing an α-tertiary stereocenter with excellent enantioselectivity.
The key to success is not only the introduction of a Cu­(I)/chiral
phosphoric acid dual-catalytic system but also the use of urea with
two acidic N–H as both the nucleophile and directing group.
The utility of this method is illustrated by facile transformations
of the products into other important compounds useful in organic synthesis
and medicinal chemistry.