Another Angewandte paper for 2025, this time with A. Arribas as first author and F. López as corresponding, is already available on-line
05/27/2025We are really pleased to announce here that our most recent research article at Angew. Chem Int. Ed., entitled "Iridium-Catalyzed Enantioselective Intramolecular Hydroarylation of Allenes: Formal Synthesis of (+)-Rhazinilam" and authored by A. Arribas, A. Rey, M. Calvelo, J. L. Mascareñas and F. López, has been accepted and it's already on-line (gold Open Access).
Abstract: We report a versatile, highly enantioselective intramolecular hydroarylation of allenyl-tethered pyrroles and indoles. The reaction, promoted by an iridium(I)/bisphosphine chiral catalyst, provides a direct access heteropolycyclic systems bearing either tertiary or quaternary carbon stereocenters and a synthetically appealing alkenyl pendant. The method allows a highly efficient assembly of five-, six- and even seven-membered fused indole and pyrrole products, providing enantiomeric excesses of up to 99%. DFT computational studies align nicely with the experimental results and allow to rationalize the key factors that control both regio- and stereoselectivity of the process. Finally, the synthetic potential of the method was exemplified with a very short, highly enantioselective formal synthesis of (+)-Rhazinilam
External link: https://onlinelibrary.wiley.com/doi/10.1002/anie.202508252