title: Synthesis of Cyclic Peptidomimetics via a Pd-Catalyzed Macroamination Reaction.
abstract: A new method to access cyclic peptidomimetics via a Pd-catalyzed macroamination reaction is presented. Natural amino acid amines are revealed as proficient coupling partners in these transformations. With a commercially available CPhos G3 catalyst system and substrates bearing diverse amino acid and aryl halide backbones, the unique head to side-chain (or side-chain mimic) macrocycles are afforded with ring sizes from 11 to 23 members in yields up to 84%.
authors: Discovery Chemistry, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors: Brett A
authors: BA
authors: Hopkins
authors: Discovery Chemistry, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors: Graham F
authors: GF
authors: Smith
authors: Discovery Chemistry, Merck Research Laboratories , 33 Avenue Louis Pasteur, Boston, Massachusetts 02115, United States.
authors: Nunzio
authors: N
authors: Sciammetta