Abstract: The direct meta⁃C-H functionalization has proved to be more challenging due to the high energy transition state of marcrocyclic metallacycles which makes its formation extremely difficult. In this paper, the reaction of allyl acetic acid alkenylation based on pyrimidine template under palladium catalysis was studied. The reaction conditions were optimized, the influences of solvent effect, catalyst and oxidant type on the reaction were investigated, and the optimal reaction conditions were obtained. The experimental results show that the designed pyrimidine⁃directed aryl acetic acid C-H bond activation reaction can realize the meta⁃selective functionalization reaction of aryl acetic acid derivatives. A meta⁃alkenylation ibuprofen derivatives with potential drug activity can be constructedby using this strategy.

Key words: Palladium catalyst, m?Methylphenylacetic, Ibuprofen, Alkenylation, Pyrimidine template

摘要： 由于反应过程中形成不稳定的大环金属中间体和较高的过渡态内能导致反应较难进行，芳烃直接间位碳氢官能化具有很大挑战性。在过渡金属钯催化条件下，研究了嘧啶模板导向的芳基乙酸间位碳氢烯基化反应。对反应条件进行优化，考察了溶剂效应、催化剂、氧化剂的种类对反应的影响，获得最佳的反应条件。结果表明，所设计的嘧啶导向的芳基乙酸碳氢键活化反应可以实现芳基乙酸衍生物的间位高选择性官能化反应，利用该策略可构建出具有潜在药物活性的间位烯基化的布洛芬衍生物。

关键词: 钯催化剂, 　间甲基苯乙酸, 　布洛芬, 　烯基化, 　嘧啶模板