Copper‐catalyzed intermolecular asymmetric propargylic amination with 4‐hydroxypyridines has been realized for the first time. In the presence of Cu complex derived from Pybox ligand, the N‐propargylated 4‐pyridones were obtained under mild reaction conditions with up to 99 % yield and 95 % ee. The Pybox ligand bearing a 4‐F‐phenyl substituent plays a key role for the high enantioselectivity. The products can be easily transformed to the core structure of quinolizidine alkaloids.

中文翻译：

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铜催化的分子间不对称炔丙基胺的高效合成N-烷基化的4-吡啶酮

首次实现了铜催化的4-羟基吡啶分子间不对称炔丙基胺化反应。在存在源自Pybox配体的Cu络合物的情况下，在温和的反应条件下可获得N炔丙基化的4-吡啶酮，收率高达99％，ee高达95％。带有4-F-苯基取代基的Pybox配体对于高对映选择性起着关键作用。该产物可以容易地转化为喹oli嗪生物碱的核心结构。