A novel protocol for the one-pot borylation/Suzuki reaction provides easy access to hinge-binding groups for kinase inhibitors. Issue 3 (1st December 2015)

• Record Type: Journal Article
• Authors: Hooper, A.; Zambon, A.; Springer, C. J.
• Is Part Of: Organic & biomolecular chemistry. Volume 14:Issue 3(2016)
• Page Start: 963
• Page End: 969
• Publication Date: 2015-12-01
• Subjects: Chemistry, Organic -- Periodicals; Bioorganic chemistry -- Periodicals; Chemistry, Physical organic -- Periodicals; 547
• DOI: 10.1039/c5ob01915j
• Languages: English
• ISSNs: 1477-0520

Abstract

Abstract : This new microwave-assisted method provides a quick one-pot borylation/Suzuki protocol that does not require additional ligands nor double loading of catalyst. Abstract : The one-pot borylation/Suzuki reaction is a very efficient means of accessing cross-coupling products of two aryl-halide partners that generally requires the use of specific catalysts or ligands and/or relatively long reaction times. This new microwave-assisted method provides a quick one-pot borylation/Suzuki reaction protocol that we applied to the synthesis of various bi- or poly-aryl scaffolds, including a variety of aryl and heteroaryl ring systems and the core frameworks of kinase inhibitors vemurafenib and GDC-0879.