过渡金属催化的单取代-1,2,3-三氮唑的C-H键功能化研究

项目名称： 过渡金属催化的单取代-1,2,3-三氮唑的C-H键功能化研究

项目编号： No.21272174

项目类型： 面上项目

立项/批准年度： 2013

项目学科： 数理科学和化学

项目作者： 匡春香

作者单位： 同济大学

项目金额： 80万元

中文摘要： 单取代-1,2,3-三氮唑是重要的药物活性基团，在医药、农药等领域已有重要应用。申请者已在1-位、2-位和4-位-单取代-1, 2, 3-三氮唑的合成及C-H活化方面做了较多前期工作，本课题拟开展过渡金属催化的单取代-1,2,3-三氮唑的C-H键功能化研究。在过渡金属存在下，以1,2,3-三氮唑为导向基团，对取代芳基上与1, 2, 3-三氮唑环相邻的C-H键进行反应，合成功能化的单取代-1,2,3-三氮唑，探讨反应机理；并对1,2,3-三氮唑母环和N-氧化1, 2, 3-三氮唑环上的C-H键进行功能化研究，合成结构新颖的1,2,3-三氮唑的衍生物。本项目将为单取代-1,2,3-三氮唑及其衍生物的合成提供新思路和新方法。对所合成的各种1,2,3-三氮唑进行吲哚胺2,3-加双氧酶（IDO）抑制活性筛选，发现高活性的IDO抑制剂，为开发高效抗肿瘤药提供先导化合物。

中文关键词： 1;2;3-三氮唑；碳氢键活化；过渡金属；衍生化；催化

英文摘要： Monosubstituted 1,2,3-triazoles, due to their unique chemical and structural properties, have received much attention over the past decades and found wide application in medicinal and pesticidal chemistry. The applicant has been concentrated in the synthesis of various types of monosubstituted 1, 2, 3-triazoles and C-H bond activation, has developed some new strategies for the preparation of 1-, 2- and 4 - monosubstituted 1, 2,3-triazoles. The present study is aimed to study the C-H bond functionalization of monosubstituted 1, 2, 3-triazole under the catalyzation of transition metal. Using 1,2,3-triazoles as oriented groups, the reaction of C-H bond in substituted aryl adjacent to the 1,2,3-triazole ring is carried out in the presence of transition metal. In this way, functionalized monosubstituted 1,2,3-triazoles are obtained, and reaction mechanism will be studied. The study of the C-H bond functionalization of 1,2,3-triazole mother ring and N-oxidation of 1, 2, 3- triazole ring will also be performed to afford various novel 1,2,3 -triazole derivatives. The project will offer new potent scientific basis and new methods for the synthesis of monosubstituted 1,2,3-triazole and its derivatives. The synthesized monosubstituted 1,2,3-triazoles will be subjected to indoleamine 2,3-dioxygenase enzyme (IDO) inhibitory

英文关键词： 1;2;3-Triazoles；C-H activation；Transition metal；Derivatization；Catalysis