A novel intramolecular macrocyclization reaction on solid support usin
g Heck reaction was achieved. The Heck coupling of acrylic acid amide
to 3-iodobenzylamine on solid support proceeds smoothly to yield a cyc
lic tetrapeptide derivative containing a new 3-substituted cinnamic ac
id template and Arg-Gly-Asp sequence. The macrocyclization reaction ta
kes place more rapidly on solid support than in solution. (C) 1997 Els
evier Science Ltd.