| abstract |
The invention also relates to a process for the synthesis of a cyclic pentapeptide ornithine-proline-D-cyclohexylalanine-tryptophan-arginine of formula A; wherein R 1 and R 2 are, independently, -H, or -C (O) R 3 , wherein R 3 is -Ch 2 Ph, -CH 2 CH 2 Ph, -CH = CHPh, -C (NHAC) CH 2 Ph; the process comprising the steps of: forming a proline-D-cyclohexylalanine-tryptophan-arginine-ornithine linear pentapeptide of formula B attached to a polymer resin; R 1 being such that for formula A, RES indicate the polymer resin, and P 1 and P 2 are protecting groups; cyclizing the linear pentapeptide of formula B to form a cyclic pentapeptide of formula C attached to the polymer resin; cleaving the cyclic peptide of formula C from the cleaved cyclic pentapeptide-providing resin having a free amine group of an ornithine residue; optionally, substitution of the free amine group of the ornithine residue of the cleaved cyclic peptide; removing the protecting groups P 1 and P 2 , to provide the cyclic peptide of formula A. |