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Beilstein Arch. 2024, 202421. https://doi.org/10.3762/bxiv.2024.21.v1
Published 12 Apr 2024
A novel Rh-catalyzed one-pot Ullmann homo-coupling reaction of Grignard reagents was achieved. The reaction with bromobenzenes having an electron-donating group or halogen group gave the corresponding homo-coupling products in good yields, although heterocyclic or aliphatic bromides did not give the products. A highly reactive Rh(III)-bis(aryl) complex would play an important role in giving the homo-coupling products in this reaction. The reaction was applied to the integrin inhibitor that was being developed in parallel. As the result, we synthesized a novel inhibitor for integrins which is critical for several diseases.
Keywords: Ullmann reaction; rhodium catalyst; homo-coupling; biphenyltetracarboxylic acid; integrin inhibitor
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Sato, K.; Teranishi, S.; Sakaue, A.; Karuo, Y.; Tarui, A.; Kawai, K.; Takeda, H.; Kinashi, T.; Omote, M. Beilstein Arch. 2024, 202421. doi:10.3762/bxiv.2024.21.v1
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