有机化学 ›› 2018, Vol. 38 ›› Issue (12): 3211-3218.DOI: 10.6023/cjoc201805022 上一篇    下一篇

所属专题: 碳氢活化合辑2018-2019

研究论文

钌(Ⅲ)催化的芳烃室温邻位羟甲基化反应

张勇, 杨中振, 余昕玲, 程旭, 李伟剑, 郭令妹, 海俐, 郭丽, 吴勇   

  1. 四川大学华西药学院 成都 610041
  • 收稿日期:2018-05-09 修回日期:2018-07-31 发布日期:2018-09-05
  • 通讯作者: 郭丽, 吴勇 E-mail:guoli@scu.edu.cn;wyong@scu.edu.cn
  • 基金资助:

    国家自然科学基金(Nos.81373259,81573286,81602954)资助项目.

Room Temperature Ru(Ⅲ)-Catalyzed ortho-Hydroxymethylation of Arenes

Zhang Yong, Yang Zhongzhen, Yu Xinling, Cheng Xu, Li Weijian, Guo Lingmei, Hai Li, Guo Li, Wu Yong   

  1. Key Laboratory of Drug-Targeting of Education Ministry and Department of Medicinal Chemistry, West China School of Pharmacy, Sichuan University, Chengdu 610041
  • Received:2018-05-09 Revised:2018-07-31 Published:2018-09-05
  • Contact: 10.6023/cjoc201805022 E-mail:guoli@scu.edu.cn;wyong@scu.edu.cn
  • Supported by:

    Project supported by the National Natural Science Foundation of China (Nos. 81373259, 81573286, 81602954).

开发了一种通过钌(Ⅲ)催化的N-导向碳氢活化反应来直接合成羟甲基化芳烃衍生物的新方法.该方法的底物适用范围广泛,室温条件下即可以较高收率制得目标产物.为化学结构中含有羟甲基的生物活性化合物的合成提供了新的思路.

关键词: 碳氢活化, 多聚甲醛, 羟甲基化, 室温

Direct synthesis of the hydroxymethylated arene derivatives via ruthenium(Ⅲ)-catalyzed nitrogen atom directed C-H activation is described. The reaction proceeds smoothly at room temperature and generates the corresponding products in moderate to excellent yields. Meanwhile, it has a broad substrate scope and opens up an attractive avenue for the application of direct hydroxymethylation in the synthesis of biologically active compounds.

Key words: C-H activation, paraformaldehyde, hydroxymethylation, room temperature