Pd0‐Catalyzed Four‐Component Reaction of Aryl Halide, CO, N‐Tosylhydrazone, and Amine.

A Pd0‐catalyzed four‐component cascade reaction of an aryl halide, CO, an N‐tosylhydrazone, and an amine affording α‐amino ketone has been developed. This reaction involves a sequential carbonylation, metal carbene migratory insertion, and amination. Control experiments and DFT calculations further reveal the reaction sequence and chemoselectivity of individual components in this cascade process. Four‐component cascade in sequence: A Pd0‐catalyzed four‐component cascade reaction of an aryl halide, CO, an N‐tosylhydrazone, and an amine follows a sequence of carbonylation, PdII carbene migratory insertion, and amination, affording α‐amino ketones in a straightforward manner. [ABSTRACT FROM AUTHOR]