Ether-Directed ortho-C–H Olefination with a Palladium(II)/Monoprotected Amino Acid Catalyst


  • We gratefully acknowledge The Scripps Research Institute, the National Institutes of Health (NIGMS, 1 R01 GM084019-04), Amgen, Novartis, and Eli Lilly for financial support. We also thank the Agency for Science, Technology and Research (A*STAR) Singapore for a postdoctoral fellowship (D.L.). L.W. is a visiting student from Nanjing University of Science and Technology, sponsored by the China Scholarship Council.


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Weak coordination is powerful! A PdII-catalyzed olefination of ortho-C[BOND]H bonds of arenes directed by weakly coordinating ethers is developed by using monoprotected amino acid (MPAA) ligands. This finding provides a method for chemically modifying ethers, which are abundant in natural products and drug molecules. HFIP=hexafluoroisopropanol.