α-取代的氮杂环结构广泛分布于具有重要生理活性的生物碱中,例如α-苄基、α-芳基和α-苯乙基取代的四氢异喹啉、四氢喹啉及哌啶等.因为不需要活性官能团的参与,通过直接对氮原子α位的C—H修饰,构建上述杂环骨架,代表了一种新的、原子经济的合成策略.但是已报道的方法的底物范围十分有限,仅仅局限于难以去保护的N-芳基四氢异喹啉和种类单一的含碳亲核试剂,反应条件也较为苛刻,极大地限制了其在合成中的应用.山东大学药学院 α-Substituted Azaheterocyclic structures are widely distributed in alkaloids of important physiological activity such as α-benzyl, α-aryl and α-phenethyl substituted tetrahydroisoquinolines, tetrahydroquinolines and piperazoles Pyridine, etc. Since no active functional groups are involved, the above heterocyclic skeleton is constructed by direct modification of the C-H at the [alpha] position of the nitrogen atom, representing a new, economically viable synthesis strategy. However, The scope of the material is very limited, only limited to difficult to protect the N-aryltetrahydroisoquinoline and a single type of carbon-containing nucleophiles, the reaction conditions are more demanding, greatly limiting its application in the synthesis of Shandong University College of Pharmacy