Palladium‐Catalyzed C(sp3)−H Functionalization at the C3 Position of l‐Pipecolinic Acid Derivatives

Abstract The study of Pd‐catalyzed arylation, alkoxylation, and acyloxylation reactions at the C3 position of l ‐pipecolinic acid derivatives to afford cis ‐disubstituted piperidines as single stereoisomers was performed. To demonstrate the utility of the reaction, compound 10 , an analogue of (−)‐3S‐3‐PPP ( 9 ) that is used as a neuroleptic drug for the treatment of schizophrenia, was synthesized featuring the arylation and radical decarboxylation reactions as key steps.