Copper-Catalyzed C-3 Functionalization of Imidazo[1,2-a]pyridines with 3-Indoleacetic Acids

作者：Wu, Yinrong; Li, Lu; Wen, Kangmei; Deng, Jie; Chen, Jiewen; Shi, Jie; Wu, Ting; Pang, Jianxin^*; Tang, Xiaodong^*

来源：Journal of Organic Chemistry, 2021, 86(17): 12394-12402.

DOI：10.1021/acs.joc.1c01371

• ALIPHATIC CARBOXYLIC-ACIDS
• REGIOSELECTIVE SULFENYLATION
• IMIDAZOHETEROCYCLES
• ARYLATION
• FLUORINATION
• AMINATION
• OXIDATION

A copper-catalyzed C-3 functionalization of imidazo[1,2-a]pyridines with 3-indoleacetic acids through an aerobic oxidative decarboxylative process has been developed. The protocol provided a series of 3-(1H-indol-3-ylmethyl)-imidazo[1,2-a]pyridines in moderate to good yields under simple reaction conditions. Importantly, some products exhibited potent antiproliferative activity in cancer cell lines.

• 单位
  南方医科大学