Journal
ADVANCED SYNTHESIS & CATALYSIS
Volume 354, Issue 10, Pages 2031-2037Publisher
WILEY-V C H VERLAG GMBH
DOI: 10.1002/adsc.201200398
Keywords
copper; cross-coupling; P ligands; synthetic methods
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Funding
- National Institutes of Health [GM46059]
- Astellas Foundation for Research on Metabolic Disorders for a Fellowship
- Grants-in-Aid for Scientific Research [11J03163] Funding Source: KAKEN
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Improved processes for the preparation of biphenyl-based phosphine ligands t-BuBrettPhos, RockPhos, and BrettPhos are presented. The new methods, featuring the use of Grignard reagents and catalytic amounts of copper, are superior to the previous methods, which require the use of tert-butyllithium and stoichiometric amounts of copper. Specifically, the use of less dangerous reagents provides a safer process, while the use of catalytic amounts of copper allows for the isolation of pure products in high yield. These improvements are particularly significant for the large-scale preparation of these ligands.
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