C-to-N atom swapping and skeletal editing in indoles and benzofurans

Abstract Skeletal editing comprises the structural reorganization of compounds. Such editing can be achieved through atom swapping, atom insertion, atom deletion or reorganization of the compound’s backbone structure 1,2 . Conducted at a late stage in drug development campaigns, skeletal editing enables diversification of an existing pharmacophore, enhancing the efficiency of drug development. Instead of constructing a heteroarene classically from basic building blocks, structural variants are readily accessible directly starting from a lead compound or approved pharmacophore. Here we present C to N atom swapping in indoles at the C2 position to give indazoles through oxidative cleavage of the indole…

• AV
  Alexander von Humboldt-Stiftung
• DF
  Deutsche Forschungsgemeinschaft
• CS
  China Scholarship Council
• WW
  Westfälische Wilhelms-Universität Münster