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Keywords:

  • amino acids;
  • C[BOND]C coupling;
  • C[BOND]H activation;
  • palladium
Thumbnail image of graphical abstract

Taking direction well: Substituted phenylalanine derivatives were prepared by C[BOND]H bond functionalization (see scheme). The syntheses are highly convergent and employ an N-phthaloylalanine with a 2-thiomethylaniline directing group. The use of an 8-aminoquinoline directing group allows for the diarylation of methyl and the diastereoselective arylation of methylene groups.