通过高通量药物筛选发现先导化合物(leading compounds)的有效性取决于化合物样品库中化合物的数量与质量，而化合物样品的质量主要由化合物结构的多样性来决定，因此，构建一个分子结构丰富，数量庞大的高品质化合物样品库是农药及医药研发的基础，也是药物合成研究的一大核心课题。本项目以“酮醛一水合物、对甲苯磺酰肼、Cs2CO3”为一个“多组分试剂系统（Multicomponent Reagents）”，历经一系列自序化的反应转化而在现场形成一个具有广泛反应活性的α-重氮酮活泼中间体,基于原位捕获与多样性导向合成策略，结合不同反应类型所需的活性功能团和各种环加成的组装原理去设计捕获子对其进行原位捕获，从而形成一个多样性导向的新型反应系统，探索出一个新型小分子化合物库的构建方法，同时，期冀为一系列碳/杂环结构体的合成建立新颖的多组分反应模式，并为相关生物活性筛选研究提供一个优质的化合物样本库

The effectiveness of discovering leading compounds by high-throughput drug screening highly depends on the number and quality of the compounds in the compound library, and the quality of the compound is primarily determined by their structural diversity. Therefore, building a compound library with large number of molecules and considerable structural diversity is not only a fundamental work for pesticide and pharmaceutical research, but also a major subject of drug synthesis. In this project, arylglyoxal monohydrate, p-toluenesulfonyl hydrazide, and cesium carbonate are treated as multicomponent reagents, in which the highly reactive α-diazoketone intermediate is formed in situ via a series of self-organized transformation. Based on the strategies of in-situ trapping and diversity-oriented synthesis (DOS), a wide variety of trappers are designed to trap the α-diazoketone intermediate. Thus, with the consideration of the requirement for functional groups and the principles of different reaction types, this project is expected to develop new types of diversity-oriented reaction systems and novel methods for the constructing of small molecule library. Moreover, new reaction modes are expected to be established for the synthesis of different carbon-heterocyclic structures, thus providing a high-quality compound library for related bioactivity studies.