Transition metal catalyzed cross-coupling of aryl Grignard reagents with aryl fluorides via Pd- or Ni-activation of the C-F bond: an efficient synthesis of unsymmetrical biaryls - application of microwave technology in ligand and catalyst screening |
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Authors: | John W Dankwardt |
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Institution: | DSM Pharmaceutical Chemicals, 5900 NW Greenville Blvd., Greenville, NC 27834, USA |
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Abstract: | Biaryl compounds are prevalent in both nature and in active pharmaceutical ingredients. The palladium and nickel catalyzed cross-coupling of aryl Grignard reagents with aryl fluorides reported herein affords moderate to excellent yields of the corresponding unsymmetrical biaryls. In addition, the first example of a biaryl cross-coupling utilizing unactivated aryl fluorides under phosphine free palladium conditions is reported. Microwave technology allowed rapid optimization of catalyst systems, which identified several ligands for this cross-coupling reaction. |
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Keywords: | Palladium Nickel Biaryls Cross-coupling Homogeneous catalysis |
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