Process for producing peptides with side chains containing imida

Chemistry: natural resins or derivatives; peptides or proteins; – Peptides of 3 to 100 amino acid residues – Chemical aftertreatment – e.g. – acylation – methylation – etc.

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530333, 530337, 530336, A61K 3800

Patent

active

054322634

ABSTRACT:
The present invention provides a process for the preparation of peptides which have or side-chains containing an alkyl- or dialkyl-substituted guanidinyl group or a imidazinylamino or tetrahydropyrimidinylamino group. The process provides higher overall yields of peptide product by permitting the synthesis of the entire peptide chain prior to modification of the side-chain to introduce the groups.

REFERENCES:
Theobald, J Am Chem Soc 112, 9624 (1990).
J. Med. Chem., Nesto, Jr., et al., "Potent Gonadotropin Releasing Hormone Antagonists with Low Histamine-Releasing Activity", pp. 3942-3948, vol. 35, published 1992.

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