Synthesis of hpGRF (Somatocrinin) in liquid phase and intermediate peptides

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United States of America Patent

PATENT NO 4581168
SERIAL NO

06580287

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Abstract

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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.

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Patent Owner(s)

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SANOFI A FRENCH CORP40 AVENUE GEORGE V PARIS 75008

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Demarne, Henri Montpellier, FR 22 87
Diaz, Joseph Perols, FR 9 43
Roncucci, Romeo Paris, FR 14 230
Schmelck, Paul-Henry Paris, FR 4 16

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