如何通过芳基的直接官能团化反应进行芳基分子修饰是合成化学的重要前沿科学问题。通过过渡金属催化来进行的的芳基间位直接官能团化反应是这类科学问题中的重要内容并且已成为合成化学界新的科学热点之一。我们以先前对于钌催化的芳基间位直接溴化方法学的研究为起点，试图发展一系列过渡金属如钌、铑、钯催化的芳基间位官能团化新合成方法。拟通过以下三个方面的内容进行深入系统性的研究：1.研究芳基过渡金属化合物的形成过程，探索金属与亲电试剂SEAr反应的基本科学理论，尤其聚焦在带有常见导向基团芳烃、非导向芳烃的SEAr反应； 2.系统的考察亲电试剂及偶联基团，发展过渡金属催化的芳基间位直接官能团化新反应方法（主要包括烷基、芳基及胺基化）；通过试验与理论计算探索反应机理；形成新的分子设计理论； 3. 以具有抗癌活性的芳基间位化合物为导向，合成具有广泛代表性的间位芳基化合物库，为将来的具有生物活性分子的筛选提供分子源。

How to use modern tools in synthetic chemistry to facilitate the synthesis of molecules in a controlled fashion is the fundamental scientific theme. The direct atom-economic synthesis of meta-C-H functionalization arenes under transition-metal catalyzed conditions is one of the challenges in organic chemistry. Based on our previous discoveries in Ru-catalyzed meta-selective arene bromination reactions, we are keen to develop a series of general synthetic methodologies via Rh, Ru or Pd-catalyzed arene direct functionalization. In this programme, we will be focusing on the 3 areas, 1. To prepared a series of aryl organometallic reagents, evaluate the SEAr processes while reacting organometallic reagents with various electrophiles; 2. Screen electrophiles as well as coupling partners, to develop new synthetic methodologies toward the meta-selective direct arene functionalizations (including alkylation, arylation and amination), to build up new concepts in molecular design; 3. Emulating by anti-cancer agents, we will build up a molecular library on meta-disubstituted arenes, these would be beneficial with regard to accessing molecular resource for the later durg discovery.