title: N-terminus 4-Chloromethyl Thiazole Peptide as a Macrocyclization Tool in the Synthesis of Cyclic Peptides: Application to the Synthesis of Conformationally Constrained RGD-Containing Integrin Ligands.
abstract: The synthesis of conformationally constrained RGD-containing integrin ligands via an efficient solid-phase intramolecular thioalkylation reaction is described. The reaction of S-nucleophiles with newly generated N-terminal 4-chloromethyl thiazoles leads to the desired cyclic RGD products 5 in high purities and good overall yields.
authors.affiliation: Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port Saint Lucie, FL 34987.
authors.forename: Adel
authors.initials: A
authors.lastname: Nefzi
authors.forename: Jason E
authors.initials: JE
authors.lastname: Fenwick