Heteroatom Annulations: The Catalytic Synthesis of Heterocycles

杂环化合物的重要性怎么强调都不过分;所有已知的有机化合物中约有一半含有杂环。这些化合物，无论是天然产物还是设计的分子，都负责各种各样的生物过程，并且它们在大多数药物中发挥作用。它们也被用作农用化学品、着色剂和新材料。杂环化合物的合成具有悠久而广泛的历史，其中已经开发了许多经典的合成方法，然而仍然存在重大挑战，某些化合物类别仍然难以制备。现代发现化学也对合成路线提出了新的要求，需要通过简单的后期修饰快速获得相关结构。在这项提案中，我们提出了新的方法，允许使用一个单一的策略访问各种杂环系统。在这个过程中，我们打开了新类别的杂环前体，也允许访问的结构，传统上提出了相当大的挑战。所提出的methodolgy结合了两个简单的建立转换，以产生一个强大的新方法杂环合成。该方法是基于串联钯催化的使用，关键是允许从单一类别的前体获得各种不同的杂环。我们还将展示如何使用这种新方法来制备极具挑战性的杂环目标系统。

The importance of heterocyclic compounds cannot be overstated; around one half of all known organic compounds contain a heterocyclic ring. These compounds, be they natural products or designed molecules, are responsible for an amazing variety of biological processes and they feature in the majority of pharmaceuticals. They are also used as agrochemicals, colourants and as new materials. The synthesis of heterocyclic compounds has a long and extensive history in which many classic syntheses have been developed, however significant challenges still remain, with certain compound classes remaining difficult to prepare. Modern discovery chemistry also places new demands on synthetic routes, requiring rapid access to related structures through simple late-stage modifications. In this proposal we present new methodology that allows access to a variety of heterocyclic systems using a single strategy. In the process we open new classes of heterocycle precursors and also allow access to structures that have traditionally presented considerable challenges.The proposed methodolgy combines two simple established transformations to generate a powerful new method for heterocycle synthesis. The method is based on the use of tandem palladium catalysis, and crucially allows a whole variety of different heterocycles to be accessed from a single class of precursor. We will also demonstrate how this new method can be used to prepared extremely challenging heterocyclic target systems.