Pd-Catalyzed Regioselective Intramolecular Allylic C-H Amination of 1,1-Disubstituted Alkenyl Amines.

Pd-Catalyzed intramolecular allylic C-H amination of 1,1-disubstituted alkenyl amines with various allylic tethers (X = O, NMs, CH 2 ) was developed. This process allows for the divergent synthesis of 1,3- X , N -heterocycles through a regioselective allylic C-H cleavage and π-allylpalladium formation. Particularly noteworthy is the use of substrates containing a labile allylic moiety and new simple catalytic systems capable of promoting highly chemo- and regioselective allylic C-H amination by overcoming significant challenges.