【摘 要】
：
手性吲哚骨架广泛存在于许多天然产物和药物活性分子中,该类骨架的催化不对称构建受到化学工作者的强烈关注1.在众多的策略中,吲哚醇和吲哚烯被认为是重要的活性试剂,可
【机 构】
：
江苏师范大学化学化工学院,徐州江苏221116
【出 处】
：
中国化学会第十三届全国有机合成化学学术研讨会
论文部分内容阅读
手性吲哚骨架广泛存在于许多天然产物和药物活性分子中,该类骨架的催化不对称构建受到化学工作者的强烈关注1.在众多的策略中,吲哚醇和吲哚烯被认为是重要的活性试剂,可以参与手性布朗斯特酸催化的不对称反应,高立体选择性地合成手性吲哚衍生物2.其中,2-吲哚烯是一类高效合成手性吲哚衍生物的多碳合成子,在大多数反应中都是作为二烯体(C4合成子)使用.我们设计了一类新型的3-烷基-2-吲哚烯,通过在吲哚C3位引入烷基,降低此位置的亲核性,从而使吲哚烯末端的双键碳更具亲核性,可以作为单烯烃(C2合成子)参与化学反应3.在这个设计基础之上,我们发展了一系列3-烷基-2-吲哚烯参与的催化不对称[n+2]环加成反应3a,b,d,以及通过反应性转换的策略实现了该类吲哚烯的催化不对称去芳构化反应3f,从而合成了多种具有立体选择性的吲哚衍生物.另一方面,我们设计了一系列吲哚醇参与的催化不对称反应4,高效高立体选择性地合成了兼具结构多样性和复杂性的手性吲哚衍生物.这里,我们将报道在这方面取得的最新研究进展.
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