title: A novel protocol for the one-pot borylation/Suzuki reaction provides easy access to hinge-binding groups for kinase inhibitors.
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.
authors.affiliation: The Institute of Cancer Research, Cancer Research UK Cancer Therapeutics Unit, Division of Cancer Therapeutics, 15 Cotswold Road, Sutton, Surrey SM2 5NG, UK. Caroline.Springer@icr.ac.uk.
authors.forename: A
authors.initials: A
authors.lastname: Hooper
authors.forename: A
authors.initials: A
authors.lastname: Zambon
authors.forename: C J
authors.initials: CJ
authors.lastname: Springer
mesh_terms: D002384:Catalysis; D004305:Dose-Response Relationship, Drug; D007192:Indenes / Q000737:chemistry; D007211:Indoles / Q000737:chemistry; D008872:Microwaves; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000737:chemistry; D010165:Palladium / Q000737:chemistry; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D011494:Protein Kinases / Q000378:metabolism*; D011720:Pyrazoles / Q000737:chemistry; D013329:Structure-Activity Relationship; D013449:Sulfonamides / Q000737:chemistry; D000077484:Vemurafenib
chemical_list: C540167:2-(4-(1-(hydroxyimino)-2,3-dihydro-1H-inden-5-yl)-3-(pyridin-4-yl)-1H-pyrazol-1-yl)ethan-1-ol; D007192:Indenes; D007211:Indoles; D009942:Organometallic Compounds; D047428:Protein Kinase Inhibitors; D011720:Pyrazoles; D013449:Sulfonamides; D000077484:Vemurafenib; D010165:Palladium; D011494:Protein Kinases