Novel peptidyl-arginine aldehyde derivatives and process for the

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2601125R, A61K 3700, C07C10352

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active

043168892

ABSTRACT:
Novel peptidyl-arginine aldehyde derivatives and their salts of formula I, ##STR1## wherein X represents a hydrogen atom, benzoyl or tert-butyloxycarbonyl group, and Y is a D-phenylalanine, .beta.-phenyl-D-lactic acid or D-allo-isoleucine moiety, are prepared from peptidyl-arginine aldehydes protected by an urethane type protecting group on their N- or O-terminal and/or a guanidino group, by removing the protecting group in a mixture of lower alkanols and water by means of hydrogenolysis, and eventually converting the product formed into a salt.
The compounds of formula I possess valuable antithrombin activity.

REFERENCES:
Chem. Abstr. vol. 83, 1975, p. 10882s.

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