Peptidylarginine aldehyde derivatives and process for the...

Details Peptidylarginine aldehyde derivatives and process for the... Peptidylarginine aldehyde derivatives and process for the...

C - Chemistry, Metallurgy

07

K

530/5.04

C07K 5/087 (2006.01) C07K 5/065 (2006.01)

Patent

CA 1133897

ABSTRACT OF THE DISCLOSURE Novel peptidyl-arginine aldehyde derivatives and their salts of general formula I or Ia Image I wherein X represents a hydrogen atom, benzoyl or tert-butyloxycarbonyl group, and Y stands for a D-phenylalanine, .beta.-phenyl-D-lactic acid or D-allo-isoleucine residue, are prepared from peptidyl-arginine aldehydes protected by an urethan type protecting group on their N- or O-terminal and/or 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 general formula I and Ia possess valuable antithrombin activity.

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