近年来, 内烯烃的烯丙基C—H键胺化反应发展迅速, 该类反应通过C—H键活化的方式高效地将氮源引入内烯烃的烯丙基位点构筑C—N键, 从而合成具有重要生物活性和药物前体的含氮化合物. 由于内烯烃活性较低, 并且在反应过程中存在化学选择性、区域选择性和立体选择性等多重挑战, 因此内烯烃的选择性烯丙基C—H键胺化反应一直是有机化学家的热门研究方向. 该综述主要介绍了近年来部分选择性内烯烃烯丙基C—H键胺化反应, 根据区分不同烯丙基C—H键的方法进行分类, 总结了该领域的研究进展及该反应在合成生物活性分子中的应用潜力.

In recent years, the allylic C—H amination of internal olefins has undergone rapid development. This reaction introduces nitrogen sources into the allylic positions of internal olefins via C—H activation efficiently to form new C—N bonds, thereby synthesizing nitrogen-containing compounds with significant biological activity and pharmaceutical potential. Given the relatively low reactivity of internal olefins and the challenges of chemoselectivity, regioselectivity and stereoselectivity during the reaction, the allylic C—H amination of internal olefins has been a great challenge for organic chemists. This review primarily covers the selective allylic C—H amination of internal olefins in recent years, categorizing the methods based on the mechanism of distinguishing different allylic C—H bonds to achieve selective amination, and summarizes the research progress in this field and its potential applications in synthesizing biologically active molecules.