Borylation via iridium catalysed C–H activation: a new concise route to duocarmycin derivatives

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The synthesis of the ethyl ester analogue of the ultrapotent antitumour antibiotic seco-duocarmycin SA has been achieved in eleven linear steps from commercially available starting materials. The DSA alkylation subunit can be made in ten linear steps from the same precursor. The route involves C–H activation at the equivalent of the C7 position on indole leading to a borylated intermediate 9 that is stable enough for peptide coupling reactions but can be easily converted to the free hydroxyl analogue.
Original languageEnglish
Pages (from-to)5603-5607
Number of pages5
JournalOrganic & Biomolecular Chemistry
Issue number27
Early online date18 Jun 2024
Publication statusPublished - 21 Jul 2024


  • Duocarmycin
  • Synthesis
  • DNA alkylation
  • C-H activation

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