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A Pd-catalyzed asymmetric allylic substitution cascade reaction, using α-(pyridin-1-yl)-acetamides (formed in situ ) as nucleophiles, has been developed, generating chiral piperidine-containing amino acid derivatives via a one-pot procedure in high yields and with up to 96% ee. The products can be easily converted into potential bioactive compounds, unnatural chiral amino acids and dipeptides.

Pd-catalyzed asymmetric allylic substitution cascade using α-(pyridin-1-yl)-acetamides formedin situas nucleophiles