手性氨基吲哚啉骨架广泛存在于天然产物和生物活性分子中，发展高效构建手性氨基吲哚啉骨架的新方法具有重要意义。近年来，过渡金属催化的吲哚不对称胺化去芳构化反应为构建手性氨基吲哚啉化合物提供了新方法，但是仍然存在着机制较单一（主要为aza-Michael加成和乃春插入）、产物结构有限等局限性。项目将利用钯催化的aza-Heck及其串联反应，以含有氮亲电试剂的吲哚衍生物为原料，通过氧化加成、迁移插入过程研究吲哚不对称胺化去芳构化，合成不同结构的手性氨基吲哚啉化合物，进一步开展一种肽模拟物和胃泌素/CCK-B受体拮抗剂(+)-AG-041R的合成研究并拓展钯催化aza-Heck及其串联反应在吡咯、呋喃等其它芳香杂环化合物的不对称胺化去芳构化中的应用。通过项目的实施，深入了解吲哚不对称胺化去芳构化的反应规律及手性诱导模式，促进吲哚不对称胺化去芳构化在含氮天然产物、药物等的合成中的应用。

Chiral aminoindoline skeleton is one of the most important building blocks, which exists extensively in natural products and biologically active compounds. Thus, novel synthetic approach to such kind of motifs is highly desirable. Recently, transition-metal-catalyzed asymmetric aminative dearomatization of indoles has been emerged as a new method to access chiral aminoindolines in spite of remaining shortcomings such as few types of mechanism (mainly through aza-Michael addition and nitrene insertion) and limited kinds of products. This project focuses on asymmetric aminative dearomatization of indoles via palladium-catalyzed aza-Heck and aza-Heck cascade reaction. Using N-electrophile containing indoles as substrates, various chiral aminoindolines can be provided through oxidative addition and following migratory insertion process. Furthermore, the synthetic application in the synthesis of a kind of peptidomimetic and potent gastrin/CCK-B receptor antagonist (+)-AG-041R will be investigated. And the asymmetric aminative dearomatization of other heteroarenes such as pyrroles and furans will be also evaluated. On the other hand, this project will study on the general rule and chirality induction mode of the asymmetric aminative dearomatization of indoles, which will ulteriorly expand its application in the synthesis of N-containing complex molecules such as natural products and pharmaceuticals.