Nickel-catalyzed mild synthesis of functional γ-amino butyric acid esters via direct α-C(sp 3 )-H allylation of N -alkyl anilines with allyl sulfones.

Herein, by employing a readily available Ni(OAc) 2 ·4H 2 O/TBHP catalyst system, we present a new method for mild synthesis of α -methylene- γ -amino butyric acid esters via direct α -C(sp 3 )-H allylation of N -alkyl anilines with allyl sulfones under oxidative nickel catalysis. The synthetic protocol proceeds with good substrate and functional group compatibility, operational simplicity, the use of base metal catalysts and easily accessible feedstocks, and no need for pre-functionalization of the α -site of N -alkyl anilines. In addition, the obtained products are applicable for further elaboration of functional molecules.