Macrocyclization on solid support using Heck reaction

Article abstract of DOI:10.1016/S0040-4039(97)01123-4

A novel intramolecular macrocyclization reaction on solid support; using Heck reaction was achieved. The Heck coupling of acrylic acid amide to 3-iodobenzylamine on solid support proceeds smoothly to yield a cyclic tetrapeptide derivative containing a new 3-substituted cinnamic acid template and Arg-Gly-Asp sequence. The macrocyclization reaction takes place more rapidly on solid support than in solution.