Synthesis of hpgrf (somatocrinin) in liquid phase and...

C - Chemistry – Metallurgy – 07 – K

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530/7.1

C07K 14/60 (2006.01) C07K 1/02 (2006.01) C07K 5/062 (2006.01) C07K 5/068 (2006.01) C07K 5/072 (2006.01) C07K 5/083 (2006.01) C07K 5/107 (2006.01) C07K 5/113 (2006.01) C07K 7/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 1267998

PATENT APPLICATION entitled: Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides in the names of: J. DIAZ H. DEMARNE R. RONCUCCI P. H. SCHMELCK assigned to: SANOFI ABSTRACT OF THE DISCLOSURE The invention relates to synthesis of hpGRF (Somatocrinin) in liquid phase and to intermediate peptides, comprising: - coupling, one after the other and in the order of the sequence of the GRF, the fragments in which: a) the side acid functions of the aspartic and glutamic acids and the side amine function of the lysine are protected by protector groups stable in the conditions of deprotection of the group Boc, b) the guanidine function of the arginine is protected by protonation, and c) the N-terminal amino acid is protected on the amine by the Boc group; - selectively eliminating the group Boc from the N-terminal amine of the peptide in phase of elongation by hydrolysis with trifluoroacetic acid, said coupling being effected in an aprotic polar solvent and - eliminating, at the end of sequence, all the protec- tor groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

447826

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