Solid phase synthesis of 'head-to-tail' cyclic peptides using a sulfonamide 'safety-catch' linker: the cleavage by cyclization approach

A new approach to the synthesis of cyclic peptides using Kenner's 'safety-c atch' sulfonamide linker is described. After the linear peptide is assemble d by Fmoc peptide synthesis, trityl is adopted as a temporary protecting gr oup for the N-terminus amine while activating the acyl sulfonamide linker. Head-to-tail cyclization-cleavage of the amine to the acyl sulfonamide ensu red final product purity. (C) 1999 Elsevier Science Ltd. All rights reserve d.