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Site‐Selective CH Borylation of Quinolines at the C8 Position Catalyzed by a Silica‐Supported Phosphane–Iridium System |
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| Authors: | Shota Konishi Dr Soichiro Kawamorita Dr Tomohiro Iwai Prof Patrick G Steel Prof?Dr Todd B Marder Prof?Dr Masaya Sawamura |
| Affiliation: | 1. Department of Chemistry, Faculty of Science, Hokkaido University, Sapporo 060‐0810 (Japan);2. Department of Chemistry, Durham University, South Road, Durham DH1 3LE (UK);3. Institut für Anorganische Chemie, Julius–Maximilians–Universit?t Würzburg, Am Hubland, 97074 Würzburg (Germany) |
| Abstract: | Site‐selective C? H borylation of quinoline derivatives at the C8 position has been achieved by using a heterogeneous Ir catalyst system based on a silica‐supported cage‐type monophosphane ligand SMAP. The efficient synthesis of a corticotropin‐releasing factor1 (CRF1) receptor antagonist based on a late‐stage C? H borylation strategy demonstrates the utility of the C8 borylation reaction. |
| Keywords: | borylation C H activation heterogeneous catalysis iridium quinoline |
