The Ullmann coupling reaction catalyzed by a highly reactive rhodium-aryl complex derived from Grignard reagent and its application

Submitting author affiliation:
Setsunan University, Hirakata, Osaka, Japan

Beilstein Arch. 2024, 202421.

Published 12 Apr 2024

cc-by Logo
This preprint has not been peer-reviewed. When a peer-reviewed version is available, this information will be updated.


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

Supporting Information

Format: DOCX Size: 914.6 KB   Download

How to Cite

When a peer-reviewed version of this preprint is available, this information will be updated in the information box above. If no peer-reviewed version is available, please cite this preprint using the following information:

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

Download Citation

Citation data can be downloaded as file using the "Download" button or used for copy/paste from the text window below.
Citation data in RIS format can be imported by all major citation management software, including EndNote, ProCite, RefWorks, and Zotero.