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<p></p><p>The high efficiency of the cobalt(II) terpyridine complex as a precatalyst in the dearomative borylation of indoles using pinacolborane as the borylation agent was demonstrated. The reaction was tested on a series of indoles bearing substituents of different nature at the C-5 position of the indole ring and with various electron-withdrawing protecting groups on the indole nitrogen. The applicability of the proposed synthetic protocol for gram-scale synthesis was also demonstrated. The resulting pinacolboranes were subsequently converted into the corresponding boron fluorides with high yields.</p>

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Efficient synthesis of 3-borylated indolines via cobalt-catalyzed dearomative borylation of indoles

  • 期刊论文

  • 发表日期：

    2026年5月13日

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  • Oleksandr V. Vashchenko,
  • Tetyana V. Bondarchuk,
  • Ilona V. Raspertova,
  • Valerii O. Bukhanko,
  • Dmytro M. Khomenko,
  • Rostyslav D. Lampeka

摘要

The high efficiency of the cobalt(II) terpyridine complex as a precatalyst in the dearomative borylation of indoles using pinacolborane as the borylation agent was demonstrated. The reaction was tested on a series of indoles bearing substituents of different nature at the C-5 position of the indole ring and with various electron-withdrawing protecting groups on the indole nitrogen. The applicability of the proposed synthetic protocol for gram-scale synthesis was also demonstrated. The resulting pinacolboranes were subsequently converted into the corresponding boron fluorides with high yields.