Asymmetric 1,2-addition of aryl boronic acids to N-carbamoyl (Cbz and Fmoc) protected glyoxylate-derived hydrazones affords α-aryl α-hydrazino esters/amides, key building blocks en route to artificial peptides.

Catalysts generated by combinations of Pd(TFA) 2 and pyridine-hydrazone ligands have been applied to 1,2 addition of arylboronic acids to aliphatic N-carbamoyl (Cbz) hydrazones, affording protected αaryl monoalkylhydrazines with high enantioselectivities (37-99% ee). Subsequent removal of the benzyloxy carbonyl protecting group provides a direct entry to free monosubstituted hydrazines, key building blocks for the synthesis of appealing 1,2-diaza-heterocycles, aminoacid derived hydrazides and other pharmacophores thereof.