杂环化合物广泛存在于药物分子中，在药物合成和发现过程中扮演着举足轻重的作用，因此，如何快速构建杂环分子骨架并高效地进行结构多样性合成，是现代有机合成化学领域中既重要又充满挑战性的工作。本项目针对并杂环化合物体系，设计巧妙的合成路线，把惰性键活化和Smiles重排反应串联起来，实现结构多样性杂环分子的快速合成与修饰，使得快速构建庞大的药物分子库成为可能。该课题的研究将对药物的筛选和发现起到有力地推动作用，也能为结构复杂的天然产物全合成提供理论指导。

Heterocyclic compounds are widely present in drug molecules and play a decisive role in drug synthesis and discovery process. How to construct a heterocyclic molecular skeleton and efficiently structure diversity oriented synthesis is an important and challenging work in modern organic chemistry. In this project, we designed an efficient synthetic strategy for the construction of fused heterocyclic system through establishing a link between inert bond activation and Smiles rearrangement, to realize the rapid synthesis and modification of molecular structural diversity, and the rapid construction of a huge library of possible drug molecules. The research of this subject will play a powerful role in promoting screening of drugs and discovery, and provide theoretical guidance for the total synthesis of complicated biological molecules and natural products.