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 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.

中文翻译：

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Pd(II)-催化芳基硼酸与脂肪族 N-氨基甲酰基腙的不对称加成

由 Pd(TFA) ₂和吡啶-腙配体组合生成的催化剂已应用于芳基硼酸与脂肪族N-氨基甲酰基 (Cbz) 腙的 1,2 加成反应，得到具有高对映选择性 (37-99%) 的受保护的 α-芳基单烷基肼ee)。随后去除苄氧基羰基保护基团可直接进入游离的单取代肼，这是合成吸引人的 1,2-二氮杂杂环、氨基酸衍生的酰肼及其其他药效团的关键构件。