2019, Do, Hoang Huy, Ullah, Saif, Villinger, Alexander, Lecka, Joanna, Sévigny, Jean, Ehlers, Peter, Iqbal, Jamshed, Langer, Peter

A two-step palladium-catalyzed procedure based on Suzuki–Miyaura cross coupling, followed by a double Buchwald–Hartwig reaction, allows for the synthesis of pharmaceutically relevant benzo[4,5]furo[3,2-b]indoles in moderate to very good yield. The synthesized compounds have been analyzed with regard to their inhibitory activity (IC50) of nucleotide pyrophosphatases h-NPP1 and h-NPP3. The activity lies in the nanomolar range. The results were rationalized based on docking studies. © 2019 Do et al.