Process for the synthesis, in liquid phase, of somatocrinin and intermediate peptides

摘要

The present invention relates to a process for the synthesis, in liquid phase and via fragments, of somatocrinin (hpGRF) according to which the following fragments are coupled successively and in the order of the GRF sequence: - 20-44 (25 alpha-amino acids) peptide K; - 5-19 (15 alpha-amino acids) peptide J; - 1-4 (4 alpha-amino acids) peptide I in which a. The acid side groups of aspartic and glutamic acids and the amine side group of lysine are protected by protecting groups which are stable under the conditions for the deprotection of the tert-butoxycarbonyl group (Boc); b. The guanidine group of arginine is protected by protonation, and c. The N-terminal amino acid of the J fragment is protected on the amino by the Boc group which is capable of being selectively removed during the GRF elongation phase by hydrolysis with trifluoroacetic acid, the couplings being carried out in an aprotic polar solvent and all the protecting groups are removed at the end of the sequence.