Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediat

Details Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediat Synthesis of hpGRF(Somatocrinin) in liquid phase and intermediat

1985-12-11

1987-11-03

Phillips, Delbert R.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

25 or more amino acid residues in defined sequence

530329, 530330, 530331, C07K 710, C07K 706, C07K 508, C07K 510

Patent

active

047044500

ABSTRACT:
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 protector groups by hydrolysis with the aid of a 0.1 to 1M solution of methanesulfonic or trifluoromethanesulfonic acid in trifluoroacetic acid.

REFERENCES:
patent: 4581168 (1986-04-01), Diaz et al.

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