Abstract

AbstractCatalysts 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 α‐aryl 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.magnified image

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