Late-stage azolation of benzylic C-H bonds enabled by electrooxidation

• 作者: Zhixiong Ruan Zhixing Huang Zhongnan Xu Shaogao Zeng Pengju Feng Ping-Hua Sun
• 来源期刊: 中国科学：化学（英文版）
• 年，卷（期）: 2021,（5）
• 所属期刊栏目: ARTICLES
• 页码范围: 800-807
• 页数: 8页
• 语种: 英文

摘要

The installation of azoles via C-H/N-H cross-coupling is significantly underdeveloped,particularly in benzylic C-H azolation due to the requirement for external chemical oxidants and the challenge in controlling the site-and chemo-selectivity.Herein,a late-stage azolation of benzylic C-H bonds enabled by electrooxidation is described,which proceeds in an undivided cell under mild,catalyst-and chemical-oxidant-free reaction conditions.The strategy empowers the C-H azolation on primary,secondary,and even challenging tertiary benzylic positions selectively.The remarkable synthetic utility of our approach is highlighted by its easy scalability without overoxidation of products and ample scope with valuable functional groups.The approach can be directly used to install benzyl and azole motifs on highly functionalized drug molecules.