Abstract Transition-metal-catalyzed sp 3 C [BOND] H activation has emerged as a powerful approach to functionalize saturated cyclic amines. Our group recently disclosed a direct catalytic arylation reaction of piperidines at the α position to the nitrogen atom. 1-(Pyridin-2- yl) piperidine could be smoothly α-arylated if treated with an arylboronic ester in the presence of a catalytic amount of [Ru 3 (CO) 12] and one equivalent of 3-ethyl-3-pentanol. ...