胺化
电泳剂
化学
钯
降冰片烯
芳基
催化作用
磷化氢
组合化学
叔胺
亲电胺化
复分解
有机化学
碘化物
药物化学
烷基
聚合
聚合物
作者
Xin Liu,Qi Zhu,Guangbin Dong
标识
DOI:10.1002/anie.202404042
摘要
Since the discovery of the palladium/norbornene (Pd/NBE)‐catalyzed ortho amination in 2013, escaping the limitation of only yielding tertiary anilines has been a long‐standing challenge in the past decade. Here, we describe that, by carefully choosing the phosphine ligand and NBE mediator, installation of a N‐mono‐alkylamino group becomes feasible. The reaction tolerates a wide range of aryl iodide substrates and various N‐mono‐tertiary alkylamine‐derived electrophiles. Both ipso alkenylation and alkynylation can be realized. The synthetic utility of this method is exemplified in the formation of primary amino group via selective deprotection and streamlined access to N‐heterocycles. Preliminary success of installing a bulky N‐secondary alkylamino group and mechanistic understanding of the decomposition pathways of mono N‐alkylamine electrophiles have been obtained.
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