4.7 Article

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

Journal

JOURNAL OF ORGANIC CHEMISTRY
Volume 86, Issue 17, Pages 12394-12402

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.1c01371

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Funding

  1. Guangdong Basic and Applied Basic Research Foundation [2021A1515010012]
  2. High-Level Talent Introduction Foundation of Southern Medical University [C1033520]

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A copper-catalyzed C-3 functionalization of imidazo[1,2-a]pyridines with 3-indoleacetic acids has been developed, providing a series of compounds with potent antiproliferative activity in cancer cell lines under simple reaction conditions.
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.

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