Breakthrough in Indole Chemistry Could Accelerate Drug Development

2025.08.25

Research

Indoles, which form the backbone of many bioactive compounds, are valuable in drug development but are difficult to modify at certain positions. Researchers at Chiba University have developed a cost-effective method using a copper-based catalyst to selectively attach alkyl groups to the C5 position, which has been especially challenging to target. This approach simplifies the synthesis of indole-based precursors and is expected to lead to the development of novel drug candidates in the future.  

  • Selective C5 modification of indoles using a copper-catalyzed reaction

    By using highly reactive carbenes and a copper–silver catalyst system, researchers have developed a method to selectively attach alkyl groups to the C5 position of indoles, which are found in bioactive compounds and are considered valuable building blocks for drug development.