Process for the preparation of peptides by solid-phase...

Details Process for the preparation of peptides by solid-phase... Process for the preparation of peptides by solid-phase...

C - Chemistry, Metallurgy

07

K

C07K 1/10 (2006.01) C07K 1/04 (2006.01)

Patent

CA 2050216

A process for the preparation of peptides of the formula (X)n-A-NH2 in which X is a natural or unnatural amino acid, aza-amino acid or imino acid, n is an integer from 1 to 50, preferably 1 to 30, and A is an aza-amino acid, and the physiologically tolerated salts thereof is described. Said process comprises the steps of converting a spacer into a form which is capable of acylation, reacting the latter with a suitable formic acid derivative and subsequently with an appropriate amino hydrazide, where appropriate, converting the protective group into a protective group which is base-labile or labile to weak acids, coupling the spacer obtained in this way to a resin, synthesizing the required peptide stepwise from the C-terminal end, subsequently cleaving the peptide off the resin and, where appropriate, converting it into physiologically tolerated salts thereof.

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